Thursday, 29 September 2016

Emcyt


Emcyt is a brand name of estramustine, approved by the FDA in the following formulation(s):


EMCYT (estramustine phosphate sodium - capsule; oral)



  • Manufacturer: PHARMACIA AND UPJOHN

    Approved Prior to Jan 1, 1982

    Strength(s): EQ 140MG PHOSPHATE [RLD]

Has a generic version of Emcyt been approved?


No. There is currently no therapeutically equivalent version of Emcyt available.


Note: Fraudulent online pharmacies may attempt to sell an illegal generic version of Emcyt. These medications may be counterfeit and potentially unsafe. If you purchase medications online, be sure you are buying from a reputable and valid online pharmacy. Ask your health care provider for advice if you are unsure about the online purchase of any medication.

See also: About generic drugs.




Related Patents

There are no current U.S. patents associated with Emcyt.

See also...

  • Emcyt Consumer Information (Wolters Kluwer)
  • Emcyt Consumer Information (Cerner Multum)
  • Emcyt Advanced Consumer Information (Micromedex)
  • Emcyt AHFS DI Monographs (ASHP)
  • Estramustine Consumer Information (Wolters Kluwer)
  • Estramustine Consumer Information (Cerner Multum)
  • Estramustine Advanced Consumer Information (Micromedex)
  • Estramustine Phosphate Sodium AHFS DI Monographs (ASHP)

Wednesday, 28 September 2016

Sumycin


Pronunciation: tet-ra-SYE-kleen
Generic Name: Tetracycline
Brand Name: Sumycin


Sumycin is used for:

Treating infections caused by certain bacteria.


Sumycin is a tetracycline antibiotic. It works by slowing the growth of sensitive bacteria by interfering with the production of proteins needed by the bacteria to grow. Slowing the bacteria's growth allows the body's defense mechanisms to destroy them.


Do NOT use Sumycin if:


  • you are allergic to any ingredient in Sumycin or other tetracycline antibiotics (eg, doxycycline)

  • you are taking acitretin or methoxyflurane

Contact your doctor or health care provider right away if any of these apply to you.



Before using Sumycin:


Some medical conditions may interact with Sumycin. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:


  • if you are pregnant, planning to become pregnant, or are breast-feeding

  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement

  • if you have allergies to medicines, foods, or other substances

  • if you have diarrhea, a stomach infection, or kidney problems

Some MEDICINES MAY INTERACT with Sumycin. Tell your health care provider if you are taking any other medicines, especially any of the following:


  • Acitretin or isotretinoin because side effects, such as increased pressure in the fluid surrounding the brain, may occur

  • Digoxin, methotrexate, methoxyflurane, or oral anticoagulants (eg, warfarin) because the risk of their side effects may be increased by Sumycin

  • Atovaquone, lithium, oral contraceptives (birth control pills), or penicillins (eg, amoxicillin) because their effectiveness may be decreased by Sumycin

This may not be a complete list of all interactions that may occur. Ask your health care provider if Sumycin may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.


How to use Sumycin:


Use Sumycin as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • Take Sumycin by mouth on an empty stomach at least 1 hour before or 2 hours after eating.

  • Take Sumycin with a full glass of water (8 oz/240 mL). Do not lie down for 30 minutes after taking Sumycin.

  • If you also take antacids containing aluminum, calcium, or magnesium; preparations containing bismuth, iron, zinc, or sodium bicarbonate; or calcium rich foods (eg, milk, dairy products, calcium-enriched juices), do not take them within 2 to 3 hours before or after taking Sumycin. Check with your doctor if you have questions.

  • To clear up your infection completely, take Sumycin for the full course of treatment. Keep taking it even if you feel better in a few days.

  • If you miss a dose of Sumycin, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Sumycin.



Important safety information:


  • Sumycin may cause dizziness or blurred vision. These effects may be worse if you take it with alcohol or certain medicines. Use Sumycin with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

  • Contact your doctor right away if stomach pain or cramps, severe diarrhea, or bloody stools occur. Do not treat diarrhea without first checking with your doctor.

  • Be sure to use Sumycin for the full course of treatment. If you do not, the medicine may not clear up your infection completely. The bacteria could also become less sensitive to this or other medicines. This could make the infection harder to treat in the future.

  • Sumycin may cause you to become sunburned more easily. Avoid the sun, sunlamps, or tanning booths until you know how you react to Sumycin. Use a sunscreen or wear protective clothing if you must be outside for more than a short time.

  • Do not use after expiration date. Outdated medicine is highly toxic to the kidneys.

  • Long-term or repeated use of Sumycin may cause a second infection. Tell your doctor if signs of a second infection occur. Your medicine may need to be changed to treat this.

  • Hormonal birth control (eg, birth control pills) may not work as well while you are using Sumycin. To prevent pregnancy, use an extra form of birth control (eg, condoms).

  • Lab tests may be performed while you use Sumycin. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

  • Use of Sumycin in CHILDREN may cause permanent discoloring of the teeth.

  • Sumycin should be used with extreme caution in CHILDREN younger than 8 years old; safety and effectiveness in these children have not been confirmed.

  • PREGNANCY and BREAST-FEEDING: Sumycin has been shown to cause harm to the fetus. If you think you may be pregnant, contact your doctor. You will need to discuss the benefits and risks of using Sumycin while you are pregnant. Sumycin is found in breast milk. Do not breast-feed while taking Sumycin.


Possible side effects of Sumycin:


All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:



Black hairy tongue; blurred vision; bulky loose stools; diarrhea; difficulty swallowing; fever; headache; hives; hoarseness; indigestion; inflammation or redness of tongue; joint pain; loss of appetite; mouth sores; nausea; rash; sensitivity to sunlight; sore throat; stomach pain; swelling and itching of the rectum.



Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); infection (fever, chills, sore throat); itching; nausea; severe skin reaction to the sun; vaginal irritation or discharge; vomiting.



This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.


See also: Sumycin side effects (in more detail)


If OVERDOSE is suspected:


Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.


Proper storage of Sumycin:

Store Sumycin at room temperature, between 68 and 77 degrees F (20 and 25 degrees C), in a tightly closed, light-resistant container. Keep away from heat, moisture, and light. Do not store in the bathroom. Keep Sumycin out of the reach of children and away from pets.


General information:


  • If you have any questions about Sumycin, please talk with your doctor, pharmacist, or other health care provider.

  • Sumycin is to be used only by the patient for whom it is prescribed. Do not share it with other people.

  • If your symptoms do not improve or if they become worse, check with your doctor.

  • Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Sumycin. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.



Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Sumycin resources


  • Sumycin Side Effects (in more detail)
  • Sumycin Use in Pregnancy & Breastfeeding
  • Drug Images
  • Sumycin Drug Interactions
  • Sumycin Support Group
  • 0 Reviews for Sumycin - Add your own review/rating


  • Sumycin Prescribing Information (FDA)

  • Sumycin Concise Consumer Information (Cerner Multum)

  • Sumycin Monograph (AHFS DI)

  • Tetracycline Prescribing Information (FDA)

  • tetracycline Mucous membrane, oral Advanced Consumer (Micromedex) - Includes Dosage Information



Compare Sumycin with other medications


  • Acne
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  • Bronchitis
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  • Bullous Pemphigoid
  • Chlamydia Infection
  • Ehrlichiosis
  • Epididymitis, Sexually Transmitted
  • Gonococcal Infection, Uncomplicated
  • Helicobacter Pylori Infection
  • Lyme Disease, Arthritis
  • Lyme Disease, Carditis
  • Lyme Disease, Erythema Chronicum Migrans
  • Lyme Disease, Neurologic
  • Lymphogranuloma Venereum
  • Nongonococcal Urethritis
  • Ocular Rosacea
  • Ornithosis
  • Pelvic Inflammatory Disease
  • Pemphigoid
  • Pemphigus
  • Pneumonia
  • Psittacosis
  • Rickettsial Infection
  • Syphilis, Early
  • Syphilis, Latent
  • Tertiary Syphilis
  • Upper Respiratory Tract Infection

Laxative Gentle Suppositories


Generic Name: bisacodyl (bis AK oh dil)

Brand Names: Alophen, Bisac-Evac, Bisco-Lax, Carters Little Pills, Correctol, Doxidan Tablet, Dulcolax Laxative, Evac-U-Gen, Ex-lax Ultra, Feen-A-Mint, Fleet Bisacodyl, Gen Lax, Gentlax Tablet, Gentle Laxative, Laxative Gentle Suppositories, Magic Bullet, Modane, Veracolate


What is Laxative Gentle Suppositories (bisacodyl)?

Bisacodyl is a laxative that stimulates bowel movements.


Bisacodyl is used to treat constipation or to empty the bowels before surgery, colonoscopy, x-rays, or other intestinal medical procedure.


Bisacodyl may also be used for other purposes not listed in this medication guide.


What is the most important information I should know about Laxative Gentle Suppositories (bisacodyl)?


Do not use bisacodyl if you have stomach (abdominal) pain, nausea, or vomiting, unless directed by a doctor.

If you notice a sudden change in bowel habits that persists over a period of 2 weeks, consult your healthcare provider before using a laxative.


Bisacodyl products should not be used for longer than one week, unless otherwise directed by your healthcare provider.

Rectal bleeding or failure to have a bowel movement after use of a laxative may indicate a more serious condition. Stop using bisacodyl and contact your healthcare provider.


What should I discuss with my healthcare provider before using Laxative Gentle Suppositories (bisacodyl)?


You should not use this medication if you are allergic to bisacodyl, or if you have:

  • severe stomach pain, nausea, or vomiting;




  • a perforated bowel;




  • a blockage in your intestines;




  • fructose or galactose intolerance;




  • an allergy to yellow food dye;




  • severe constipation or dehydration;




  • inflammatory bowel disease, toxic megacolon; or




  • a sudden change in bowel habits lasting 2 weeks or longer.



People with eating disorders (such as anorexia or bulimia) should not use this medication without the advice of a doctor.


If you have any of these other conditions, you may need a dose adjustment or special tests to safely use bisacodyl:



  • kidney disease;




  • trouble swallowing;




  • a history of bowel obstruction, diverticulitis, ulcerative colitis, or other intestinal disorder; or




  • if you are taking a diuretic ("water pill").




Do not use bisacodyl without telling your doctor if you are pregnant. Do not use bisacodyl without telling your doctor if you are breast-feeding a baby. Do not give this medication to a child without the advice of a doctor.

When used to treat constipation, bisacodyl is only part of a complete program of treatment that may also include diet and exercise. Follow your doctor's instructions very closely.


How should I use Laxative Gentle Suppositories (bisacodyl)?


Use this medication exactly as directed on the label, or as prescribed by your doctor. Do not use it in larger amounts or for longer than recommended.


For best results, take bisacodyl on an empty stomach, or at bedtime. Do not crush, chew, or break the enteric-coated tablet. Swallow it whole. The enteric-coated pill has a special coating to protect your stomach. Breaking the pill could damage this coating. Do not take a bisacodyl rectal (enema or suppository) by mouth. It is for use only in your rectum.

Try to use the rectal form of this medicine at a time when you can lie down afterward and hold the medicine in. Avoid using the bathroom during this time.


If you are using bisacodyl before surgery or a medical procedure, follow your doctor's instructions about the timing of your dose (the number of days or hours) before your procedure.

Remove the outer wrapper from the suppository before inserting it. Avoid handling the suppository too long or it will melt in your hands.


Lie on your side and gently insert the suppository pointed end first. For best results, hold in the suppository for a 15 to 20 minutes. The suppository will melt quickly once inserted and you should feel little or no discomfort while holding it in. Avoid using the bathroom just after you have inserted the suppository.


Shake the rectal enema gently just before use. Remove the protective cap from the applicator tip. You may use the enema lying down or seated on a toilet. Gently insert the tip into your rectum and lightly squeeze the bottle to release the enema. Hold the enema in for a few minutes and then release into the toilet.


The rectal forms of bisacodyl should produce a bowel movement within 15 minutes to 1 hour.


The tablet form of bisacodyl should produce a bowel movement within 6 to 12 hours, or overnight when taken at bedtime.


Call your doctor if you do not have a bowel movement after using this medication. Do not use bisacodyl for more than 7 days in a row unless your doctor tells you to. Store bisacodyl at room temperature away from moisture and heat.

What happens if I miss a dose?


Since bisacodyl is used only once or as needed, you are not likely to be on a dosing schedule.


What happens if I overdose?


Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include watery diarrhea, stomach cramps, muscle weakness, or urinating less than usual.


What should I avoid while using Laxative Gentle Suppositories (bisacodyl)?


Avoid using any other medications within 2 hours before or after using bisacodyl.


Avoid drinking milk within 1 hour after using bisacodyl.

Laxative Gentle Suppositories (bisacodyl) side effects


Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:

  • urinating less than usual or not at all;




  • drowsiness, confusion, mood changes, increased thirst, loss of appetite, nausea and vomiting;




  • swelling, weight gain, feeling short of breath;




  • rectal bleeding;




  • severe stomach pain or cramps, severe or ongoing diarrhea or vomiting; or




  • low potassium (confusion, uneven heart rate, extreme thirst, increased urination, leg discomfort, muscle weakness or limp feeling).



Less serious side effects may include:



  • dizziness, weakness;




  • increased thirst;




  • mild stomach pain, gas, indigestion;




  • diarrhea or loose stools;




  • mild nausea; or




  • skin rash.



This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.


What other drugs will affect Laxative Gentle Suppositories (bisacodyl)?


There may be other drugs that can interact with bisacodyl. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.



More Laxative Gentle Suppositories resources


  • Laxative Gentle Suppositories Side Effects (in more detail)
  • Laxative Gentle Suppositories Use in Pregnancy & Breastfeeding
  • Laxative Gentle Suppositories Drug Interactions
  • 0 Reviews for Laxative Gentle - Add your own review/rating


  • Bisacodyl Prescribing Information (FDA)

  • Bisacodyl Professional Patient Advice (Wolters Kluwer)

  • Bisacodyl Monograph (AHFS DI)

  • Bisacodyl MedFacts Consumer Leaflet (Wolters Kluwer)

  • Evac-u-gen Chewable Tablets MedFacts Consumer Leaflet (Wolters Kluwer)



Compare Laxative Gentle Suppositories with other medications


  • Bowel Preparation
  • Constipation


Where can I get more information?


  • Your pharmacist can provide more information about bisacodyl.

See also: Laxative Gentle side effects (in more detail)


Tuesday, 27 September 2016

Lucentis


Pronunciation: RA-ni-BIZ-oo-mab
Generic Name: Ranibizumab
Brand Name: Lucentis


Lucentis is used for:

Treating neovascular (wet) age-related macular degeneration (AMD). It is also used for treating another certain eye problem known as macular edema following retinal vein occlusion (RVO).


Lucentis is a selective vascular endothelial growth factor (VEGF) antagonist. It works by decreasing the growth of certain cells in the eye. It also helps to keep blood vessels in the eye from leaking and decreases the formation of new blood vessels in the eye. This slows or stops wet AMD and macular edema following RVO.


Do NOT use Lucentis if:


  • you are allergic to any ingredient in Lucentis

  • you have an infection in or around the eye

Contact your doctor or health care provider right away if any of these apply to you.



Before using Lucentis:


Some medical conditions may interact with Lucentis. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:


  • if you are pregnant, planning to become pregnant, or are breast-feeding

  • if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement

  • if you have allergies to medicines, foods, or other substances

  • if your condition has also been treated with a certain type of light therapy (verteporfin photodynamic therapy)

  • if you have a history of glaucoma or other eye problems

Some MEDICINES MAY INTERACT with Lucentis. However, no specific interactions with Lucentis are known at this time.


Ask your health care provider if Lucentis may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.


How to use Lucentis:


Use Lucentis as directed by your doctor. Check the label on the medicine for exact dosing instructions.


  • Lucentis is usually given as an injection into the eye at your doctor's office, hospital, or clinic.

  • Do not use Lucentis if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.

  • Lucentis is for injection into the eye only.

  • If you miss a dose of Lucentis, contact your doctor right away.


Important safety information:


  • Lucentis may cause vision changes. Do not drive, operate machinery, or do anything else that could be dangerous until you know how you react to Lucentis.

  • If you develop eye pain or redness, eye or eyelid swelling, sensitivity to light, or vision changes (eg, decreased vision), contact your doctor right away.

  • Lab tests, including eye exams and eye pressure measurements, may be performed while you use Lucentis. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.

  • Lucentis should be used with extreme caution in CHILDREN; safety and effectiveness in children have not been confirmed.

  • PREGNANCY and BREAST-FEEDING: It is not known if Lucentis can cause harm to the fetus. If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Lucentis while you are pregnant. It is not known if Lucentis is found in breast milk. If you are or will be breast-feeding while you use Lucentis, check with your doctor. Discuss any possible risks to your baby.


Possible side effects of Lucentis:


All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:



Dry eye; eye discomfort; feeling of something in the eye; headache; increased tears; nausea; nose or throat irritation; seeing floaters or spots.



Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); chest, jaw, or left arm pain; decreased vision or other vision changes; eye or eyelid swelling; eye pain, pressure, redness, bleeding, or discharge; sensitivity to light; symptoms of infection (eg, fever, chills, persistent sore throat); symptoms of a stroke (eg, one-sided weakness, slurred speech, confusion).



This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.


See also: Lucentis side effects (in more detail)


If OVERDOSE is suspected:


Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include eye swelling. Lucentis may be harmful if swallowed.


Proper storage of Lucentis:

Lucentis is usually handled and stored by a health care provider. If you are using Lucentis at home, store Lucentis as directed by your pharmacist or health care provider. Keep Lucentis out of the reach of children and away from pets.


General information:


  • If you have any questions about Lucentis, please talk with your doctor, pharmacist, or other health care provider.

  • Lucentis is to be used only by the patient for whom it is prescribed. Do not share it with other people.

  • If your symptoms do not improve or if they become worse, check with your doctor.

  • Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Lucentis. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.



Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Lucentis resources


  • Lucentis Side Effects (in more detail)
  • Lucentis Use in Pregnancy & Breastfeeding
  • Lucentis Drug Interactions
  • Lucentis Support Group
  • 1 Review for Lucentis - Add your own review/rating


  • Lucentis Prescribing Information (FDA)

  • Lucentis Monograph (AHFS DI)

  • Lucentis Advanced Consumer (Micromedex) - Includes Dosage Information

  • Lucentis Consumer Overview



Compare Lucentis with other medications


  • Diabetic Retinopathy
  • Macular Degeneration
  • Macular Edema

Monday, 26 September 2016

Atenolo Denk




Atenolo Denk may be available in the countries listed below.


Ingredient matches for Atenolo Denk



Atenolol

Atenolol is reported as an ingredient of Atenolo Denk in the following countries:


  • Ethiopia

International Drug Name Search

Friday, 23 September 2016

Lofibra



fenofibrate

Dosage Form: tablet, film coated
Lofibra® (fenofibrate tablets), 54 mg and 160 mg

691

692

Rx only

Lofibra Description


Lofibra® (fenofibrate tablets) is a lipid regulating agent available as tablets for oral administration. Each tablet contains 54 mg or 160 mg of fenofibrate. The chemical name for fenofibrate is 2-[4-(4-chlorobenzoyl) phenoxy]-2-methyl-propanoic acid, 1-methylethyl ester with the following structural formula:



C20H21O4Cl M.W. 360.83


Fenofibrate is insoluble in water. The melting point is 79 to 82°C. Fenofibrate is a white solid which is stable under ordinary conditions.


Each 54 mg Lofibra® tablet contains the following inactive ingredients: colloidal silicone dioxide, croscarmellose sodium, crospovidone, iron oxide yellow, lactose monohydrate, lecithin, microcrystalline cellulose, polyvinyl alcohol, povidone, sodium lauryl sulfate, sodium starch glycolate, sodium stearyl fumarate, talc, titanium dioxide, xanthan gum, and D&C yellow #10 lake.


Each 160 mg Lofibra® tablet contains the following inactive ingredients: colloidal silicone dioxide, croscarmellose sodium, crospovidone, lactose monohydrate, lecithin, microcrystalline cellulose, polyvinyl alcohol, povidone, sodium lauryl sulfate, sodium starch glycolate, sodium stearyl fumarate, talc, titanium dioxide, and xanthan gum.



Lofibra - Clinical Pharmacology


A variety of clinical studies have demonstrated that elevated levels of total cholesterol (total-C), low density lipoprotein cholesterol (LDL-C), and apolipoprotein B (apo B), an LDL membrane complex, are associated with human atherosclerosis. Similarly, decreased levels of high density lipoprotein cholesterol (HDL-C) and its transport complex, apolipoprotein A (apo AI and apo AII) are associated with the development of atherosclerosis. Epidemiologic investigations have established that cardiovascular morbidity and mortality vary directly with the level of total-C, LDL-C, and triglycerides, and inversely with the level of HDL-C. The independent effect of raising HDL-C or lowering triglycerides (TG) on the risk of cardiovascular morbidity and mortality has not been determined.


Fenofibric acid, the active metabolite of fenofibrate, produces reductions in total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides and triglyceride rich lipoprotein (VLDL) in treated patients. In addition, treatment with fenofibrate results in increases in high density lipoprotein (HDL) and apoproteins apoAI and apoAII.


The effects of fenofibric acid seen in clinical practice have been explained in vivo in transgenic mice and in vitro in human hepatocyte cultures by the activation of peroxisome proliferator activated receptor α (PPARα). Through this mechanism, fenofibrate increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III (an inhibitor of lipoprotein lipase activity).


The resulting fall in triglycerides produces an alteration in the size and composition of LDL from small, dense particles (which are thought to be atherogenic due to their susceptibility to oxidation), to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly. Activation of PPARα also induces an increase in the synthesis of apoproteins A-I, A-II and HDL-cholesterol.


Fenofibrate also reduces serum uric acid levels in hyperuricemic and normal individuals by increasing the urinary excretion of uric acid.



Pharmacokinetics/Metabolism


Plasma concentrations of fenofibric acid after administration of three 48 mg or one 145 mg tablets are equivalent under fed conditions to one 200 mg capsule.


Absorption

The absolute bioavailability of fenofibrate cannot be determined as the compound is virtually insoluble in aqueous media suitable for injection. However, fenofibrate is well absorbed from the gastrointestinal tract. Following oral administration in healthy volunteers, approximately 60% of a single dose of radiolabelled fenofibrate appeared in urine, primarily as fenofibric acid and its glucuronate conjugate, and 25% was excreted in the feces. Peak plasma levels of fenofibric acid occur within 6 to 8 hours after administration.


Exposure to fenofibric acid in plasma, as measured by Cmax and AUC, is not significantly different when a single 145 mg dose of fenofibrate is administered under fasting or nonfasting conditions.


Distribution

Upon multiple dosing of fenofibrate, fenofibric acid steady state is achieved within 9 days. Plasma concentrations of fenofibric acid at steady state are approximately double those following a single dose. Serum protein binding was approximately 99% in normal and hyperlipidemic subjects.


Metabolism

Following oral administration, fenofibrate is rapidly hydrolyzed by esterases to the active metabolite, fenofibric acid; no unchanged fenofibrate is detected in plasma.


Fenofibric acid is primarily conjugated with glucuronic acid and then excreted in urine. A small amount of fenofibric acid is reduced at the carbonyl moiety to a benzhydrol metabolite which is, in turn, conjugated with glucuronic acid and excreted in urine.


In vivo metabolism data indicate that neither fenofibrate nor fenofibric acid undergo oxidative metabolism (e.g., cytochrome P450) to a significant extent.


Excretion

After absorption, fenofibrate is mainly excreted in the urine in the form of metabolites, primarily fenofibric acid and fenofibric acid glucuronide. After administration of radiolabelled fenofibrate, approximately 60% of the dose appeared in the urine and 25% was excreted in the feces.


Fenofibric acid is eliminated with a half-life of 20 hours, allowing once daily administration in a clinical setting.



Special Populations


Geriatrics

In elderly volunteers 77 to 87 years of age, the oral clearance of fenofibric acid following a single oral dose of fenofibrate was 1.2 L/h, which compares to 1.1 L/h in young adults. This indicates that a similar dosage regimen can be used in the elderly, without increasing accumulation of the drug or metabolites.


Pediatrics

Fenofibrate has not been investigated in adequate and well-controlled trials in pediatric patients.


Gender

No pharmacokinetic difference between males and females has been observed for fenofibrate.


Race

The influence of race on the pharmacokinetics of fenofibrate has not been studied, however fenofibrate is not metabolized by enzymes known for exhibiting inter-ethnic variability. Therefore, inter-ethnic pharmacokinetic differences are very unlikely.


Renal Insufficiency

The pharmacokinetics of fenofibric acid was examined in patients with mild, moderate, and severe renal impairment. Patients with severe renal impairment (creatinine clearance [CrCl] ≤ 30 mL/min) showed 2.7 fold increase in exposure for fenofibric acid and increased accumulation of fenofibric acid during chronic dosing compared to that of healthy subjects. Patients with mild to moderate renal impairment (CrCl 30 to 80 mL/min) had similar exposure but an increase in the half-life for fenofibric acid compared to that of healthy subjects. Based on these findings, the use of fenofibrate should be avoided in patients who have severe renal impairment and dose reduction is required in patients having mild to moderate renal impairment.


Hepatic Insufficiency

No pharmacokinetic studies have been conducted in patients having hepatic insufficiency.


Drug-drug Interactions

In vitro studies using human liver microsomes indicate that fenofibrate and fenofibric acid are not inhibitors of cytochrome (CYP) P450 isoforms CYP3A4, CYP2D6, CYP2E1, or CYP1A2. They are weak inhibitors of CYP2C8, CYP2C19 and CYP2A6, and mild-to-moderate inhibitors of CYP2C9 at therapeutic concentrations.


Potentiation of coumarin-type anticoagulants has been observed with prolongation of the prothrombin time/INR.


Bile acid sequestrants have been shown to bind other drugs given concurrently. Therefore, fenofibrate should be taken at least 1 hour before or 4 to 6 hours after a bile acid binding resin to avoid impeding its absorption (see WARNINGS and PRECAUTIONS).


Concomitant administration of a single dose of fenofibrate (administered as 3 X 67 mg fenofibrate micronized capsules) with a single dose of pravastatin (40 mg) in 23 healthy subjects increased the mean Cmax and mean AUC for pravastatin by 13%. The Cmax and AUC of fenofibrate decreased by 2% and 1%, respectively, after concomitant administration of fenofibrate and pravastatin. The mean Cmax and AUC for 3α-hydroxy-iso-pravastatin increased by 29% and 26%, respectively.


Concomitant administration of a single dose of fenofibrate (equivalent to 145 mg fenofibrate) and a single dose of fluvastatin (40 mg) resulted in a small increase (approximately 15 to 16%) in exposure to (+)3R,5S-fluvastatin, the active enantiomer of fluvastatin.


A single dose of either pravastatin or fluvastatin had no clinically important effect on the pharmacokinetics of fenofibric acid.


Concomitant administration of fenofibrate (equivalent to fenofibrate 145 mg) with atorvastatin (20 mg) once daily for 10 days resulted in approximately 17% decrease (range from 67% decrease to 44% increase) in atorvastatin AUC values in 22 healthy males. The atorvastatin Cmax values were not significantly affected by fenofibrate. The pharmacokinetics of fenofibric acid were not significantly affected by atorvastatin.


Concomitant administration of fenofibrate (equivalent to fenofibrate 145 mg) once daily for 10 days with glimepiride (1 mg tablet) single dose simultaneously with the last dose of fenofibrate resulted in a 35% increase in mean AUC of glimepiride in healthy subjects. Glimepiride Cmax was not significantly affected by fenofibrate coadministration. There was no statistically significant effect of multiple doses of fenofibrate on glucose nadir or AUC with the baseline glucose concentration as the covariate after glimepiride administration in healthy volunteers. However, glucose concentrations at 24 hours remained statistically significantly lower after pretreatment with fenofibrate than with glimepiride alone. Glimepiride had no significant effect on the pharmacokinetics of fenofibric acid.


Concomitant administration of fenofibrate (54 mg) and metformin (850 mg) three times a day for 10 days resulted in no significant changes in the pharmacokinetics of fenofibric acid and metformin when compared with the two drugs administered alone in healthy subjects.


Concomitant administration of fenofibrate (equivalent to fenofibrate 145 mg) once daily for 14 days with rosiglitazone tablet (rosiglitazone maleate) (8 mg) once daily for 5 days, Day 10 through Day 14, resulted in no significant changes in the pharmacokinetics of fenofibric acid and rosiglitazone when compared with the two drugs administered alone in healthy subjects.



Clinical Trials


Hypercholesterolemia (Heterozygous Familial and Nonfamilial) and Mixed Dyslipidemia (Fredrickson Types IIa and IIb)

The effects of fenofibrate at a dose equivalent to 145 mg per day were assessed from four randomized, placebo-controlled, double-blind, parallel-group studies including patients with the following mean baseline lipid values: total-C 306.9 mg/dL; LDL-C 213.8 mg/dL; HDL-C 52.3 mg/dL; and triglycerides 191.0 mg/dL. Fenofibrate therapy lowered LDL-C, Total-C, and the LDL-C/HDL-C ratio. Fenofibrate therapy also lowered triglycerides and raised HDL-C (see Table 1).






































































Table 1. Mean Percent Change in Lipid Parameters at End of Treatment*

*

Duration of study treatment was 3 to 6 months.


p = < 0.05 vs. Placebo

Treatment GroupTotal-CLDL-CHDL-CTG
Pooled Cohort
Mean baseline lipid values (n = 646)306.9 mg/dL213.8 mg/dL52.3 mg/dL191.0 mg/dL
All FEN (n = 361)-18.7%-20.6%+11.0%-28.9%
Placebo (n = 285)-0.4%-2.2%+0.7%+7.7%
Baseline LDL-C > 160 mg/dL and TG < 150 mg/dL (Type IIa)
Mean baseline lipid values (n = 334)307.7 mg/dL227.7 mg/dL58.1 mg/dL101.7 mg/dL
All FEN (n = 193)-22.4%-31.4%+9.8%-23.5%
Placebo (n = 141)+0.2%-2.2%+2.6%+11.7 %
Baseline LDL-C > 160 mg/dL and TG ≥ 150 mg/dL (Type IIb)
Mean baseline lipid values (n = 242)312.8 mg/dL219.8 mg/dL46.7 mg/dL231.9 mg/dL
All FEN (n = 126)-16.8%-20.1%+14.6%-35.9%
Placebo (n = 116)-3.0%-6.6%+2.3%+0.9%

In a subset of the subjects, measurements of apo B were conducted. Fenofibrate treatment significantly reduced apo B from baseline to endpoint as compared with placebo (-25.1% vs. 2.4%, p < 0.0001, n = 213 and 143 respectively).


Hypertriglyceridemia (Fredrickson Type IV and V)

The effects of fenofibrate on serum triglycerides were studied in two randomized, double-blind, placebo-controlled clinical trials1 of 147 hypertriglyceridemic patients (Fredrickson Types IV and V). Patients were treated for eight weeks under protocols that differed only in that one entered patients with baseline triglyceride (TG) levels of 500 to 1500 mg/dL, and the other TG levels of 350 to 500 mg/dL. In patients with hypertriglyceridemia and normal cholesterolemia with or without hyperchylomicronemia (Type IV/V hyperlipidemia), treatment with fenofibrate at dosages equivalent to fenofibate 145 mg per day decreased primarily very low density lipoprotein (VLDL) triglycerides and VLDL cholesterol. Treatment of patients with Type IV hyperlipoproteinemia and elevated triglycerides often results in an increase of low density lipoprotein (LDL) cholesterol (see Table 2).









































































































































Table 2: Effects of Fenofibrate in Patients With Fredrickson Type IV/V Hyperlipidemia

*

= p < 0.05 vs. Placebo

Study 1PlaceboFenofibrate
Baseline TG levels 350 to 499 mg/dL  N Baseline (Mean) Endpoint(Mean)% Change(Mean)  N Baseline (Mean) Endpoint(Mean)% Change(Mean)
Triglycerides28449450-0.527432223-46.2*
VLDL Triglycerides193673502.719350178-44.1*
Total Cholesterol282552612.827252227-9.1*
HDL Cholesterol283536427344019.6*
LDL Cholesterol28120129122712813714.5
VLDL Cholesterol2799995.8279246-44.7*
Study 2PlaceboFenofibrate
Baseline TG levels 500 to 1500 mg/dL  N Baseline(Mean) Endpoint(Mean)% Change(Mean)  N Baseline(Mean) Endpoint(Mean)% Change(Mean)
Triglycerides447107507.248726308-54.5*
VLDL Triglycerides2953757118.733543205-50.6*
Total Cholesterol442722710.448261223-13.8*
HDL Cholesterol4427285.048303622.9*
LDL Cholesterol4210090-4.24510313145.0*
VLDL Cholesterol4213714211.04512654-49.4*

The effect of fenofibrate on cardiovascular morbidity and mortality has not been determined.



Indications and Usage for Lofibra



Treatment of Hypercholesterolemia


Lofibra® (fenofibrate tablets) is indicated as adjunctive therapy to diet to reduce elevated LDL-C, Total-C, Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb). Lipid-altering agents should be used in addition to a diet restricted in saturated fat and cholesterol when response to diet and non-pharmacological interventions alone has been inadequate (see National Cholesterol Education Program [NCEP] Treatment Guidelines, below).



Treatment of Hypertriglyceridemia


Lofibra® (fenofibrate tablets) is also indicated as adjunctive therapy to diet for treatment of adult patients with hypertriglyceridemia (Fredrickson Types IV and V hyperlipidemia). Improving glycemic control in diabetic patients showing fasting chylomicronemia will usually reduce fasting triglycerides and eliminate chylomicronemia thereby obviating the need for pharmacologic intervention.


Markedly elevated levels of serum triglycerides (e.g., > 2,000 mg/dL) may increase the risk of developing pancreatitis. The effect of fenofibrate therapy on reducing this risk has not been adequately studied.


Drug therapy is not indicated for patients with Type I hyperlipoproteinemia, who have elevations of chylomicrons and plasma triglycerides, but who have normal levels of very low density lipoprotein (VLDL). Inspection of plasma refrigerated for 14 hours is helpful in distinguishing Types I, IV and V hyperlipoproteinemia2.


The initial treatment for dyslipidemia is dietary therapy specific for the type of lipoprotein abnormality. Excess body weight and excess alcoholic intake may be important factors in hypertriglyceridemia and should be addressed prior to any drug therapy. Physical exercise can be an important ancillary measure. Diseases contributory to hyperlipidemia, such as hypothyroidism or diabetes mellitus should be looked for and adequately treated. Estrogen therapy, thiazide diuretics and beta-blockers, are sometimes associated with massive rises in plasma triglycerides, especially in subjects with familial hypertriglyceridemia. In such cases, discontinuation of the specific etiologic agent may obviate the need for specific drug therapy of hypertriglyceridemia.


The use of drugs should be considered only when reasonable attempts have been made to obtain satisfactory results with non-drug methods. If the decision is made to use drugs, the patient should be instructed that this does not reduce the importance of adhering to diet (see WARNINGS and PRECAUTIONS).


































Fredrickson Classification of Hyperlipoproteinemias
Lipid Elevation
TypeLipoprotein ElevatedMajorMinor
I (rare)chylomicronsTG↑↔C
IIaLDLC-
IIbLDL, VLDLCTG
III (rare)IDLC, TG-
IVVLDLTG↑↔C
V (rare)chylomicrons, VLDLTG↑↔C

C = cholesterol


TG = triglycerides


LDL = low density lipoprotein


VLDL = very low density lipoprotein


IDL = intermediate density lipoprotein





















NCEP Treatment Guidelines: LDL-C Goals and Cutpoints for Therapeutic Lifestyle Changes and Drug Therapy in Different Risk Categories

*

CHD = coronary heart disease


Some authorities recommend use of LDL-lowering drugs in this category if an LDL-C level of < 100 mg/dL cannot be achieved by therapeutic lifestyle changes. Others prefer use of drugs that primarily modify triglycerides and HDL-C, e.g., nicotinic acid or fibrate. Clinical judgement also may call for deferring drug therapy in this subcategory.


Almost all people with 0 to 1 risk factor have 10 year risk < 10%; thus, 10 year risk assessment in people with 0 to 1 risk factor is not necessary.

Risk Category LDL Goal (mg/dL)LDL Level at Which to Initiate Therapeutic Lifestyle Changes (mg/dL)LDL Level at Which to Consider Drug Therapy (mg/dL)
CHD* or CHD risk equivalents (10 year risk > 20%)< 100≥ 100≥ 130 (100 to 129: drug optional)
2+ Risk Factors (10 year risk ≤ 20%)< 130≥ 13010 year risk 10% to 20%: ≥ 130 10 year risk < 10%: ≥ 160
0 to 1 Risk Factor< 160≥ 160≥ 190 (160 to 189: LDL-lowering drug optional)

After the LDL-C goal has been achieved, if the TG is still ≥ 200 mg/dL, non HDL-C (total-C minus HDL-C) becomes a secondary target of therapy. Non-HDL-C goals are set 30 mg/dL higher than LDL-C goals for each risk category.



Contraindications


Lofibra® is contraindicated in patients who exhibit hypersensitivity to fenofibrate.


Lofibra® is contraindicated in patients with hepatic or severe renal dysfunction, including primary biliary cirrhosis, and patients with unexplained persistent liver function abnormality.


Lofibra® is contraindicated in patients with preexisting gallbladder disease (see WARNINGS).



Warnings



Liver Function


Fenofibrate at doses equivalent to 96 mg to 145 mg fenofibrate per day has been associated with increases in serum transaminases [AST (SGOT) or ALT (SGPT)]. In a pooled analysis of 10 placebo-controlled trials, increases to > 3 times the upper limit of normal occurred in 5.3% of patients taking fenofibrate versus 1.1% of patients treated with placebo.


When transaminase determinations were followed either after discontinuation of treatment or during continued treatment, a return to normal limits was usually observed. The incidence of increases in transaminases related to fenofibrate therapy appear to be dose related. In an 8 week dose-ranging study, the incidence of ALT or AST elevations to at least three times the upper limit of normal was 13% in patients receiving dosages equivalent to 96 mg to 145 mg fenofibrate per day and was 0% in those receiving dosages equivalent to 48 mg or less fenofibrate per day, or placebo. Hepatocellular, chronic active and cholestatic hepatitis associated with fenofibrate therapy have been reported after exposures of weeks to several years. In extremely rare cases, cirrhosis has been reported in association with chronic active hepatitis.


Regular periodic monitoring of liver function, including serum ALT (SGPT) should be performed for the duration of therapy with fenofibrate, and therapy discontinued if enzyme levels persist above three times the normal limit.



Cholelithiasis


Fenofibrate, like cLofibrate and gemfibrozil, may increase cholesterol excretion into the bile, leading to cholelithiasis. If cholelithiasis is suspected, gallbladder studies are indicated. Fenofibrate therapy should be discontinued if gallstones are found.



Concomitant Oral Anticoagulants


Caution should be exercised when anticoagulants are given in conjunction with fenofibrate because of the potentiation of coumarin-type anticoagulants in prolonging the prothrombin time/INR. The dosage of the anticoagulant should be reduced to maintain the prothrombin time/INR at the desired level to prevent bleeding complications. Frequent prothrombin time/INR determinations are advisable until it has been definitely determined that the prothrombin time/INR has stabilized.



Concomitant HMG-CoA Reductase Inhibitors


The combined use of fenofibrate and HMG-CoA reductase inhibitors should be avoided unless the benefit of further alterations in lipid levels is likely to outweigh the increased risk of this drug combination.


Concomitant administration of fenofibrate (equivalent to fenofibrate 145 mg) and pravastatin (40 mg) once daily for 10 days increased the mean Cmax and AUC values for pravastatin by 36% (range from 69% decrease to 321% increase) and 28% (range from 54% decrease to 128% increase), respectively, and for 3α-hydroxy-iso-pravastatin by 55% (range from 32% decrease to 314% increase) and 39% (range from 24% decrease to 261% increase), respectively (see also CLINICAL PHARMACOLOGY,  Drug-drug Interactions).


The combined use of fibric acid derivatives and HMG-CoA reductase inhibitors has been associated, in the absence of a marked pharmacokinetic interaction, in numerous case reports, with rhabdomyolysis, markedly elevated creatine kinase (CK) levels and myoglobinuria, leading in a high proportion of cases to acute renal failure.


The use of fibrates alone, including fenofibrate, may occasionally be associated with myositis, myopathy, or rhabdomyolysis. Patients receiving fenofibrate and complaining of muscle pain, tenderness, or weakness should have prompt medical evaluation for myopathy, including serum creatine kinase level determination. If myopathy/myositis is suspected or diagnosed, fenofibrate therapy should be stopped.



Mortality


The effect of fenofibrate on coronary heart disease morbidity and mortality and non-cardiovascular mortality has not been established.



Other Considerations


The Fenofibrate Intervention and Event Lowering in Diabetes (FIELD) study was a 5 year randomized, placebo-controlled study of 9795 patients with type 2 diabetes mellitus treated with fenofibrate. Fenofibrate demonstrated a non-significant 11% relative reduction in the primary outcome of coronary heart disease events (hazard ratio [HR] 0.89, 95% CI 0.75 to 1.05, p = 0.16) and a significant 11% reduction in the secondary outcome of total cardiovascular disease events (HR 0.89 [0.80 to 0.99], p = 0.04). There was a non-significant 11% (HR 1.11 [0.95, 1.29], p = 0.18) and 19% (HR 1.19 [0.90, 1.57], p = 0.22) increase in total and coronary heart disease mortality, respectively, with fenofibrate as compared to placebo.


In the Coronary Drug Project, a large study of post myocardial infarction of patients treated for 5 years with cLofibrate, there was no difference in mortality seen between the cLofibrate group and the placebo group. There was however, a difference in the rate of cholelithiasis and cholecystitis requiring surgery between the two groups (3.0% vs. 1.8%).


Because of chemical, pharmacological, and clinical similarities between fenofibrate tablets, cLofibrate, and gemfibrozil, the adverse findings in 4 large randomized, placebo-controlled clinical studies with these other fibrate drugs may also apply to fenofibrate.


In a study conducted by the World Health Organization (WHO), 5000 subjects without known coronary artery disease were treated with placebo or cLofibrate for 5 years and followed for an additional one year. There was a statistically significant, higher age-adjusted all-cause mortality in the cLofibrate group compared with the placebo group (5.70% vs. 3.96%, p = < 0.01). Excess mortality was due to a 33% increase in non-cardiovascular causes, including malignancy, post-cholecystectomy complications, and pancreatitis. This appeared to confirm the higher risk of gallbladder disease seen in cLofibrate-treated patients studied in the Coronary Drug Project.


The Helsinki Heart Study was a large (n = 4081) study of middle-aged men without a history of coronary artery disease. Subjects received either placebo or gemfibrozil for 5 years, with a 3.5 year open extension afterward. Total mortality was numerically higher in the gemfibrozil randomization group but did not achieve statistical significance (p = 0.19, 95% confidence interval for relative risk G:P = .91 to 1.64). Although cancer deaths trended higher in the gemfibrozil group (p = 0.11), cancers (excluding basal cell carcinoma) were diagnosed with equal frequency in both study groups. Due to the limited size of the study, the relative risk of death from any cause was not shown to be different than that seen in the 9 year follow-up data from World Health Organization study (RR = 1.29). Similarly, the numerical excess of gallbladder surgeries in the gemfibrozil group did not differ statistically from that observed in the WHO study.


A secondary prevention component of the Helsinki Heart Study enrolled middle-aged men excluded from the primary prevention study because of known or suspected coronary heart disease. Subjects received gemfibrozil or placebo for 5 years. Although cardiac deaths trended higher in the gemfibrozil group, this was not statistically significant (hazard ratio 2.2, 95% confidence interval: 0.94 to 5.05). The rate of gallbladder surgery was not statistically significant between study groups, but did trend higher in the gemfibrozil group, (1.9% vs. 0.3%, p = 0.07). There was a statistically significant difference in the number of appendectomies in the gemfibrozil group (6/311 vs. 0/317, p = 0.029).



Precautions



General


Initial Therapy

Laboratory studies should be done to ascertain that the lipid levels are consistently abnormal before instituting fenofibrate therapy. Every attempt should be made to control serum lipids with appropriate diet, exercise, weight loss in obese patients, and control of any medical problems such as diabetes mellitus and hypothyroidism that are contributing to the lipid abnormalities. Medications known to exacerbate hypertriglyceridemia (beta-blockers, thiazides, estrogens) should be discontinued or changed if possible prior to consideration of triglyceride-lowering drug therapy.


Continued Therapy

Periodic determination of serum lipids should be obtained during initial therapy in order to establish the lowest effective dose of Lofibra® (fenofibrate tablets). Therapy should be withdrawn in patients who do not hav

Paracetamol Mundogen




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Loratadine



Class: Second Generation Antihistamines
ATC Class: R06AX13
VA Class: AH109
Chemical Name: 4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyr idin-11-ylidene)-1-piperidinecarboxylateethyl ester
Molecular Formula: C22H23ClN2O2
CAS Number: 79794-75-5
Brands: Alavert, Claritin, Claritin-D

Introduction

Second generation antihistamine;1 2 3 4 5 6 7 8 9 10 36 37 45 46 derivative of azatadine.7 10 31 37 44


Uses for Loratadine


Allergic Rhinitis


Self-medication for symptomatic relief (alone or in fixed combination with pseudoephedrine sulfate) of seasonal allergic rhinitis (e.g., hay fever);1 3 4 5 7 8 18 19 44 67 70 71 72 73 74 75 76 77 use fixed combination preparations only when both antihistamine and nasal decongestant activity are desired.18 19


As effective as astemizole (no longer commercially available in the US),4 7 39 azatadine,10 39 chlorpheniramine,7 39 clemastine,4 7 37 39 or terfenadine (no longer commercially available in the US).4 5 7 21 37 39


Has been used for the symptomatic treatment of perennial allergic rhinitis.39


Chronic Idiopathic Urticaria


Self-medication for symptomatic relief of pruritus, erythema, and urticaria associated with chronic idiopathic urticaria (e.g., hives);1 15 16 17 21 78 not for prevention of chronic idiopathic urticaria or allergic skin reactions.78


Loratadine Dosage and Administration


Administration


Oral Administration


Administer conventional tablets, orally disintegrating tablets, and fixed-combination tablets orally1 2 3 4 5 6 7 8 18 19 67 70 71 72 73 74 76 77 without regard to meals.1 18 20


Orally disintegrating tablets: Place tablet on the tongue, allow it to disintegrate (within a few seconds), then swallow with or without water.1 68 71


Fixed-combination loratadine/pseudoephedrine tablets: Swallow whole; do not break, crush, chew, or dissolve.18 19 70 73 75 76 Administer Claritin-D 24 Hour tablets with a full glass of water.19 70


Dosage


Fixed-combination tablets formulated for 12-hour dosing contain 5 mg of loratadine and 60 mg of pseudoephedrine sulfate in an immediate-release outer shell and 60 mg of pseudoephedrine sulfate in an extended-release matrix core that slowly releases the drug.18


Fixed-combination tablets formulated for 24-hour dosing contain 10 mg of loratadine in an immediate-release outer shell and 240 mg of pseudoephedrine sulfate in an extended-release matrix core that slowly releases the drug.19 20


Pediatric Patients


Allergic Rhinitis

Oral

Self-medication in children 2 to <6 years of age:65 66 5 mg once daily (as oral solution).1 72


Self-medication in children ≥6 years of age:65 66 10 mg once daily (as conventional or orally disintegrating tablets or oral solution).1 5 7 10 67 68 69 74 77


Self-medication in children ≥12 years of age:65 66 5 mg every 12 hours (in fixed combination with 120 mg pseudoephedrine sulfate as the 12-hour formulation [e.g., Alavert Allergy & Sinus, Claritin-D 12 Hour])18 73 75 76 or 10 mg once daily (in fixed combination with 240 mg pseudoephedrine sulfate as the 24-hour formulation [Claritin-D 24 Hour]).19 70


Chronic Idiopathic Urticaria

Oral

Children 2–5 years of age: Not recommended for self-medication;78 a dosage of 5 mg once daily (as oral solution) has been recommended when clinicians prescribe the drug in children 2–5 years of age.1


Self-medication in children ≥6 years of age: 10 mg once daily.1 78


Adults


Allergic Rhinitis

Oral

Self-medication:65 66 10 mg once daily (as conventional or orally disintegrating tablets or oral solution).1 5 7 10 67 68 69 74 77


Self-medication: 5 mg every 12 hours (in fixed combination with 120 mg pseudoephedrine sulfate as the 12-hour formulation)18 73 75 76 or 10 mg once daily (in fixed combination with 240 mg pseudoephedrine sulfate as the 24-hour formulation).19 70


Chronic Idiopathic Urticaria

Oral

Self-medication: 10 mg once daily.1 78


Prescribing Limits


Pediatric Patients


Allergic Rhinitis

Oral

Self-medication65 66 in children 2 to <6 years of age: Maximum 5 mg once daily (as oral solution).72


Self-medication65 66 in children ≥6 years of age: Maximum 10 mg once daily (as conventional or orally disintegrating tablets or oral solution).67 68 71 77


Self-medication in children ≥12 years of age: Maximum 10 mg daily (in fixed combination with pseudoephedrine sulfate as the 12-hour or 24-hour formulations).70 73 76


Adults


Allergic Rhinitis

Oral

Self-medication65 66 : Maximum 10 mg once daily (as conventional or orally disintegrating tablets or oral solution).67 68 71 77


Self-medication: Maximum 10 mg daily (in fixed combination with pseudoephedrine sulfate as the 12-hour or 24-hour formulations).70 73 76


Special Populations


Hepatic Impairment


Self-medication: Consult a clinician.67 70 71 72 78


Children 2–5 years of age with hepatic failure: 5 mg every other day (as oral solution).1


Adults and children ≥6 years of age with hepatic failure: 10 mg every other day (as conventional or orally disintegrating tablets or oral solution).1 18


Fixed-combination loratadine/pseudoephedrine sulfate preparations generally should not be used in patients with hepatic impairment.18 19


Renal Impairment


Self-medication: Consult a clinician.67 70 71 72 78


Children 2–5 years of age with renal insufficiency (glomerular filtration rate <30 mL/minute): 5 mg every other day (as oral solution).1


Adults and children ≥6 years of age with renal insufficiency (glomerular filtration rate <30 mL/minute): 10 mg every other day (as conventional or orally disintegrating tablets or oral solution).1 18


Fixed-combination loratadine/pseudoephedrine sulfate preparations in adults and children ≥12 years of age with renal insufficiency (glomerular filtration rate <30 mL/minute): 5 mg of loratadine once daily (when the 12-hour formulation is used) or 10 mg of loratadine every other day (when the 24-hour formulation is used).18 19


Cautions for Loratadine


Contraindications



  • Known hypersensitivity to loratadine or any ingredient in the formulation.1 18 19



Warnings/Precautions


Warnings


Phenylketonuria

Alavert orally disintegrating tablets contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 8.4 mg of phenylalanine per tablet.68


Sensitivity Reactions


Possible rash.1 Urticaria, pruritus, purpura, photosensitivity reaction, erythema multiforme, and anaphylaxis reported rarely.1 18 19


General Precautions


Use of Fixed Combinations

When using fixed-combination preparation containing pseudoephedrine sulfate, consider the cautions, precautions, and contraindications associated with pseudoephedrine.18 19


GI Obstruction and Esophageal Perforation

Mechanical upper GI obstruction and esophageal perforation reported rarely with a previously marketed formulation of Claritin-D 24 Hour tablets;19 30 individuals with a history of difficulty in swallowing tablets, a known upper GI narrowing, or abnormal esophageal peristalsis should not use the Claritin-D 24 Hour preparation since it is not known whether the currently commercially available formulation has potential for this effect.19 30


Specific Populations


Pregnancy

Category B.1 18 19


Lactation

Loratadine and its active metabolite desloratadine distribute readily into milk; pseudoephedrine (a component of fixed combination preparations) also distributes into milk.1 18 19 Caution advised; discontinue nursing or the drug.1 18 19


Pediatric Use

Safety and efficacy of loratadine alone or in fixed combination with pseudoephedrine sulfate not established in children <2 or <12 years of age, respectively.1 18 19


Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection.83 84 Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established.83 Therefore, FDA recommended not to use such preparations in children <2 years of age; safety and efficacy in older children currently under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 years of age”). FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.


Geriatric Use

Conventional or orally disintegrating tablets or oral solution: Risk of somnolence.1 Because geriatric patients frequently have decreased renal function, evaluate renal function prior to initiation and subsequently thereafter in this age group; adjust dosage if renal impairment exists or develops.1


Fixed-combination loratadine/pseudoephedrine sulfate preparations: Safety and efficacy not studied in patients ≥60 years of age.18 19 Geriatric patients are more likely to have adverse effects from sympathomimetic amines than younger patients.18 19


Hepatic Impairment

Conventional or orally disintegrating tablets or oral solution: Dosage adjustment recommended.1 (See Hepatic Impairment under Dosage and Administration.)


Fixed-combination loratadine/pseudoephedrine sulfate preparations: Use not recommended.18 19


Renal Impairment

Conventional or orally disintegrating tablets or oral solution: Dosage adjustment recommended.1 (See Renal Impairment under Dosage and Administration.)


Fixed-combination loratadine/pseudoephedrine preparations: Dosage adjustment recommended.18 19 (See Renal Impairment under Dosage and Administration.)


Common Adverse Effects


Children 2–5 years of age receiving oral solution: Diarrhea, epistaxis, pharyngitis, flu-like symptoms, fatigue, stomatitis, tooth disorder, earache, viral infection, rash.1


Children 6–12 years of age receiving oral solution: Nervousness, wheezing, fatigue, hyperkinesia, abdominal pain, conjunctivitis, dysphonia, upper respiratory tract infection.1


Adults and children ≥12 years of age receiving conventional or orally disintegrating tablets: Headache, somnolence, fatigue, dry mouth.1


Fixed combination loratadine/pseudoephedrine sulfate preparations: Insomnia, dry mouth, headache, somnolence, nervousness, dizziness, fatigue.18 19


Interactions for Loratadine


Metabolized principally by CYP3A4 and to lesser extent by CYP2D6.1 39


No formal drug interaction studies conducted with fixed combination loratadine/pseudoephedrine preparations.18 19 When using these preparations, consider drug interactions associated with pseudoephedrine.18 19


Drugs Affecting Hepatic Microsomal Enzymes


Inhibitors of CYP3A4 or CYP2D6: Potential pharmacokinetic interaction (increased plasma concentrations of loratadine and desloratadine).1 18 19 39 64 (See Specific Drugs under Interactions.)


Specific Drugs















Drug



Interaction



Comments



Cimetidine



Increased loratadine and desloratadine concentrations; no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects reported1 18 19 39 64



Ketoconazole



Increased loratadine and desloratadine concentrations; no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects reported1 18 19 39 64



Macrolide antibiotics (e.g., clarithromycin, erythromycin)



Increased loratadine and desloratadine concentrations; no clinically important changes in ECG or laboratory evaluations, vital signs, or adverse effects reported1 18 19 39 64


Loratadine Pharmacokinetics


Absorption


Bioavailability


Rapidly absorbed from the GI tract following oral administration;1 10 18 19 37 38 39 42 49 in animal studies, 85% of an oral dose was absorbed.7 41 43 Peak plasma concentrations are attained in about 1.5–3.7 hours.10


Onset


Antihistaminic effect is apparent within 1–4 hours.1 10 18 19 36 39


Duration


Antihistaminic effect persists for 12–24 hours.1 2 10 18 19 38 46 61


Food


Food increases the extent of loratadine absorption and delays time to peak plasma concentration by about 1 hour.1 18 19


Special Populations


In patients with hepatic impairment, increased peak plasma loratadine concentrations and AUC secondary to impaired drug metabolism can occur.1 7 10 18 19 39


In patients with chronic renal impairment (Clcr ≤30 mL/minute), peak plasma concentrations and AUC of loratadine and desloratadine are increased compared with those in adults with normal renal function.1 4 18 19 38


In geriatric patients, peak plasma concentrations and AUC of loratadine and desloratadine are increased compared to those in younger adults.1 18 19


Distribution


Extent


Distribution has not been determined.10 Neither the drug nor its metabolites appear to cross the blood-brain barrier.1 18 19 Loratadine and its metabolites are distributed into breast milk in concentrations that are equivalent to plasma concentrations.1 7 10 18 19 40


Plasma Protein Binding


97–99% (loratadine); 73–77% (desloratadine).7 10 18 19 39 40


Elimination


Metabolism


Extensive first-pass metabolism by CYP enzymes in the liver to the active desloratadine metabolite.1 18 19 39 41 44 49 50 Metabolized principally by CYP3A4 and to lesser extent by CYP2D6.1 39


Elimination Route


Excreted equally in urine and feces as metabolic products.1 18 19


Half-life


The mean distribution half-life of loratadine is about 1–2 hours;7 10 37 41 42 the mean elimination half-life is 8–15 hours.1 7 10 18 19 37 41 42 44 49 The mean distribution half-life of desloratadine is about 2–4 hours;7 10 41 42 the mean elimination half-life is 17–28 hours.1 7 10 18 19 41 42 44 49


Special Populations


In patients with hepatic impairment, elimination half-life of loratadine and desloratadine is increased with increasing severity of hepatic disease.1 7 10 18 19 39


In patients with renal impairment (Clcr ≤30 mL/minute), mean elimination half-lives of loratadine and desloratadine appear to be similar to those in patients with normal renal function.1 4 10 18 19 39 43


In a limited number of geriatric patients (66–78 years of age), half-lives of loratadine and desloratadine were increased compared to those in younger adults.1 18 19


Stability


Storage


Oral


Tablets

2–30°C.1 Protect from excessive moisture.67 77 78


Orally Disintegrating Tablets

2–25°C.68 71 Use tablet immediately after opening individual blister; use within 6 months of opening foil pouch.71


Solution

2–25°C.72


Fixed-Combination Tablets

15–25°C.70 73 76


ActionsActions



  • Exhibits specific, selective peripheral H1-receptor antagonistic activity.1 2 3 4 5 6 7 8 9 10 36 37 45 46




  • No appreciable anticholinergic7 10 49 or α-adrenergic blocking7 10 37 51 activity in vitro.




  • In clinical studies, incidence of CNS effects (e.g., sedation, impaired psychomotor performance) associated with loratadine is similar to that with placebo or terfenadine (no longer commercially in the US) and less than that with first generation antihistamines (e.g., azatadine, chlorpheniramine, clemastine).1 7 10 18 19 37



Advice to Patients



  • For self-medication, importance of taking only as needed and not exceeding recommended dosage; taking more than recommended dosage may cause drowsiness.67 68 70 71 72 73 76 77




  • For self-medication with loratadine in fixed combination with pseudoephedrine, importance of discontinuing therapy and contacting a clinician if symptoms do not improve within 7 days or are accompanied by fever, or if nervousness, dizziness, or sleeplessness occurs.70 73 76




  • For self-medication for management of chronic idiopathic urticaria (e.g., hives), importance of understanding that loratadine does not prevent hives.78 Importance of consulting a clinician before initiating therapy if hives are unusual in color, look bruised or blistered, or do not itch.78 Importance of discontinuing therapy and contacting a clinician if symptoms do not improve within 3 days or if hives have persisted for >6 weeks.78




  • Importance of understanding that chronic idiopathic urticaria may present with other severe allergic reactions, including anaphylactic shock (e.g., trouble swallowing, swelling of the tongue, trouble speaking, wheezing or trouble breathing, dizziness or loss of consciousness, swelling in or around the mouth, drooling).78 These manifestations may occur when hives first appear or up to several hours later and can be life-threatening if not treated immediately.78 Importance of immediately seeking emergency help if anaphylactic shock occurs.78 If an epinephrine auto-injector has been prescribed, importance of carrying this device at all times; never use loratadine as a substitute for the epinephrine auto-injector.78




  • Importance of discontinuing the drug immediately and informing a clinician if an allergic or hypersensitivity reaction occurs.67 68 69 70 71 72 73 77




  • Importance of informing patients with phenylketonuria that some orally disintegrating tablet preparations (e.g. Alavert) contain aspartame.68




  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1




  • Importance of patients with renal or hepatic impairment, heart disease, hypertension, thyroid disease, diabetes mellitus, or difficulty in urination resulting from prostate enlargement not undertaking self-medication without first consulting a clinician.1 70 73 75 (See Cautions.)




  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1




  • Importance of informing patients of other important precautionary information.1 (See Cautions.)



Preparations


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.


* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name











































Loratadine

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Oral



Solution



5 mg/5 mL



Children's Claritin Fruit Flavored Syrup 24 Hour



Schering-Plough



Children’s Claritin Allergy, Grape Flavor



Schering-Plough



Tablets



10 mg*



Alavert Non-Drowsy Allergy Relief 24 Hour



Wyeth



Claritin Hives Relief



Schering-Plough



Claritin 24 Hour



Schering-Plough



Tablets, orally disintegrating



10 mg



Alavert Non-Drowsy Allergy Relief 24 Hour



Wyeth



Claritin Reditabs 24 Hour



Schering-Plough























Loratadine Combinations

Routes



Dosage Forms



Strengths



Brand Names



Manufacturer



Oral



Tablets, extended-release core (containing pseudoephedrine 60 mg)



5 mg with Pseudoephedrine Sulfate 120 mg



Alavert Allergy & Sinus D-12 Hour



Wyeth



Claritin-D 12 Hour



Schering-Plough



Tablets, extended-release core (pseudoephedrine sulfate only), film-coated



10 mg with Pseudoephedrine Sulfate 240 mg



Claritin-D 24 Hour



Schering-Plough


Comparative Pricing


This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.


Claritin 10MG Tablets (SCHERING-PLOUGH HEALTHCARE): 30/$30.99 or 90/$70.97


Claritin 10MG Tablets (SCHERING-PLOUGH HEALTHCARE): 30/$35.99 or 90/$89.97


Claritin Reditabs 10MG Dispersible Tablets (SCHERING-PLOUGH HEALTHCARE): 10/$20.99 or 30/$41.97


Loratadine 10MG Tablets (SANDOZ): 30/$21.99 or 90/$60.97



Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.


The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions November 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.


† Use is not currently included in the labeling approved by the US Food and Drug Administration.




References



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3. Oei HD. Double-blind comparison of loratadine (SCH 29851), astemizole, and placebo in hay fever with special regard to onset of action. Ann Allergy. 1988; 61:436-9. [IDIS 310134] [PubMed 2904776]



4. Quercia RA, Broisman L. Focus on loratadine: a new second-generation nonsedating H1-receptor antagonist. Hosp Formul. 1993; 28:137-53.



5. Del Carpio JD, Kabbash L, Turenne Y et al. Efficacy and safety of loratadine (10 mg once daily), terfenadine (60 mg twice daily), and placebo in the treatment of seasonal allergic rhinitis. J Allergy Clin Immunol. 1989; 84:741-6. [IDIS 309183] [PubMed 2572617]



6. Simons FER. The antiallergic effects of antihistamines (H1-receptor antagonists). J Allergy Clin Immunol. 1992; 90:705-15. [IDIS 303368] [PubMed 1383310]



7. Barenholtz AH, McLeod DC. Loratadine: a nonsedating antihistamine with once-daily dosing. DICP. 1989; 23:445-50. [IDIS 254798] [PubMed 2525847]



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14. Douglas WW. Histamine and 5-hydroxytryptamine (serotonin) and their antagonists. In: Gilman AG, Goodman LS, Rall TW et al, eds. Goodman and Gilman’s the pharmacologic basis of therapeutics. 7th ed. New York: Macmillan Publishing Company; 1985:605-38.



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17. Belaich B, Bruttmann D, DeGreef H et al. Comparative effects of loratadine and terfenadine in the treatment of chronic idiopathic urticaria. Ann Allergy. 1990; 64:191-4. [IDIS 297021] [PubMed 1967919]



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19. Schering Corp. Claritin-D 24 Hour (loratadine and pseudoephedrine sulfate) extended-release tablets prescribing information. Kenilworth, NJ; 1998 Apr.



20. Schering Corp, Kenilworth, NJ: Personal communication.



21. Lutsky BN, Klose P, Melon J et al. A comparative study of the efficacy and safety of loratadine syrup and terfenadine suspension in the treatment of 3- to 6-year-old children with seasonal allergic rhinitis. Clin Ther. 1993; 15:855-65. [PubMed 8269452]



22. Meltzer EO, Weiler JM, Widlitz MD. Comparative outdoor study of the efficacy, onset and duration of action, and safety of cetirizine, loratadine, and placebo for seasonal allergic rhinitis. J Allergy Clin Immunol. 1996; 97:617-26. [IDIS 360732] [PubMed 8621847]



23. Simons FER. Hl-Receptor antagonists: comparative tolerability and safety. Drug Saf. 1994; 10:350-80. [IDIS 359177] [PubMed 7913608]



24. Gosselin RE, Smith RP, Hodge HC. Clinical toxicology of commercial products. 5th ed. Baltimore: Williams & Wilkins; 1984:I10,III-36-40.



25. Cirillo VJ, Tempero KF. The pharmacology and therapeutic use of H1 and H2 antihistamines. In: Miller RR, Greenblatt DJ, eds. Drug therapy reviews. Vol 2. New York: Elsevier/North Holland Inc; 1979:24-47.



26. AMA Division of Drugs. AMA drug evaluations. 5th ed. Chicago: American Medical Association; 1983:1465-79.



27. Church JA. Allergic rhinitis: diagnosis and management. Clin Pediatr. (Philadelphia). 1980; 19:655-9.



28. Food and Drug Administration. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; tentative final monograph for OTC antihistamine drug products. [21 FR Part 341] Fed Regist. 1985; 50:2200-18. (IDIS 195256)



29. Holgate S. Comparative trial of two non-sedative H1 antihistamines, terfenadine and astemizole, for hay fever. Thorax. 1985; 40:399.



30. Harris AG. Dear doctor letter regarding mechanical upper GI obstruction with Claritin-D 24 Hour tablets. Kenilworth, NJ: Schering Corporation; 1997 Jul.



31. Villani FJ, Magatti CV, Vashi DB et al. N-substituted 11-(4-piperidylene)-5,6-dihydro-11H-benzo-[5,6]cyclohepta[1,2b]pyrid ines. Antihistamines with no sedating liability. Arzneimittelforschung. 1986; 36:1311-4. [PubMed 2947582]



32. IorioLC, Cohen-Winston M, Barnett A. Interaction studies in mice of SCH 29851, a potential non-sedating antihistamine, with commonly used therapeutic agents. Agents Actions. 1986; 18:485-93. [PubMed 2945410]



33. Sorkin EM, Heel RC. Terfenadine: a review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1985; 29:34-56. [IDIS 197286] [PubMed 2857636]



34. Moser L, Huther KJ, Koch-Weser J et al. Effects of terfenadine and diphenhydramine alone or in combination with diazepam or alcohol on psychomotor performance and subjective feelings. Eur J Clin Pharmacol. 1978; 14:417-23. (IDIS 110254)



35. Bousquet J, Chanal I, Skassa-Brociek W et al. Lack of subsensitivity to loratadine during long-term dosing during 12 weeks. J Allergy Clin Immunol. 1990; 86:248-53. [IDIS 287716] [PubMed 1974561]



36. Roman IJ, Kassem N, Gural RP et al. Suppression of histamine-induced wheal response by loratadine (SCH 29851) over 28 days in man. Ann Allergy. 1986; 57:253-6. [IDIS 223656] [PubMed 2945499]



37. Dockhorn RJ, Bergner A, Connell JT et al. Safety and efficacy of loratadine (Sch- 29851): a new non-sedating antihistamine in seasonal allergic rhinitis. Ann Allergy. 1987; 58:407-11. [IDIS 316934] [PubMed 2954497]



38. Desager J, Horsmans Y. Pharmacokinetic-pharmacodynamic relationships of H1- antihistamines. Clin Pharmacokinet. 1995; 28:419-32. [IDIS 360835] [PubMed 7614779]



39. Haria M, Fitton A, Peters DH. Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs. 1994; 48:617-37. [IDIS 359175] [PubMed 7528133]



40. Hilbert J, Radwanski E, Affrime MB et al. Excretion of loratadine in breast milk. J Clin Pharmacol. 1988; 28:234-9. [IDIS 239877] [PubMed 2966185]