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Posts Tagged ‘tilade’

Cromolyn, Cyclobenzaprine, Cyclosporine, Darunavir

Monday, August 3rd, 2009

Generic Name
Cromolyn (KROE-inuh-lin) [9
Brand Names
Crolom    Intal
Gastrocrom    Opticrom
The information in this profile also applies to the following drugs:
Nedocromil
Alocril    Tilade
Type of Drug
Allergy preventive and antiastk)m-aft_.
Prescribed For
Prevention of severe allergic reactions, including asthma, runny nose, and mastocytosis; also prescribed for food allergies, eczema, dermatitis, chronic itching, and hay fever. It may be used to treat and prevent chronic inflammatory bowel disease. The eyedrops are used to treat conjunctivitis (pinkeye) and other eye irritations.
General Information
Unlike antihistamines, which work against histamine that has been released into the system, cromolyn sodium prevents allergy, asthma, and other conditions by stabilizing mast cells, a key component in any allergic reaction because they release histamine. Cromolyn prevents the release of histamine and other chemicals from mast cells. The drug works only in the areas to which it is applied; only 7-8% of an inhaled dose and 1 % of a swallowed capsule is absorbed into the blood. Even the oral capsules, which one would normally expect to be absorbed into the blood, treat only gastrointestinal -tract allergies. Cromolyn products must be used on a regular basis to be effective in reducing the frequency and intensity of allergic reactions.
Cautions and Warnings
Do not take cromolyn if you are allergic or sensitive to any of its ingredients. Rarely, people have experienced severe allergic attacks after taking cromolyn.
cromolyn should never be used to treat an acute allergy attack. It is intended only to prevent or reduce the number of allergic attacks and their intensity. Once the proper dosage level has been established for you, reducing that level may result in a recurrence of attacks.
People with kidney or liver disease require reduced dosage.
Cough or bronchial spasm may occasionally occur after the inhalation of a cromolyn dose. Severe bronchospasm is rare.
cromolyn aerosol should be used with caution in people with abnormal heart rhythm or diseased coronary blood vessels because of a possible reaction to the propellants used in the product.
Possible Side Effects
V Most common: rash and itching. Headache and diarrhea (for capsules). Watery, itchy, dry, or puffy eyes; and iztjes (for eyedrops). Most capsule and eyedrop side effects are mkw and may be attributable to the underlying condition; a variety have been reported but cannot be tied conclusively to the drug.
V Less common: local irritation, including nasal stinging, sneezing, tearing, cough, and stuffy nose; urinary difficulty or frequency; dizziness; headache; joint swelling; muscle Possible Side Effects (continued)
pain-, a bad taste in the mouth; sore throat-, nosebleeds’, abdominal pain-, and nausea.
♦ Rare: severe drug reactions, consisting of coughing, difficulty in swallowing, hives, itching, breathing difficulties, or swelling of the eyelids, lips, or face. Contact your doctor if you experience any side effect not listed above.
Drug Interactions None known.
Food Interactions
Inhaled or swallowed cromolyn products should not be mixed with any food, juice, or milk. The nasal and eye products may be taken without regard to food or meals.
Usual Dose
Inhaled Capsules or Solution
Adult and Child (age 2 and over): starting close-20 mg 4 times a day. Children under age 5 may inhale cromolyn powder if their allergies are severe. The solution must be given with a power-operated nebulizer and face mask. Handheld nebulizers are not adequate. To prevent exercise asthma, 20 mg may be inhaled up to 1 hour before exercise.
Aerosol
Adult and Child (age 5 and over): up to 2 sprays 4 times a day, spaced equally throughout the day. To prevent exercise asthma, 2 puffs may be inhaled up to 1 hour before exercise.
Nasal Solution
Adult and Child (age 6 and over): 1 spray in each nostril 3-6 times a day at regular intervals. First blow your nose, and then inhale the spray.
Oral Capsules
MAI and Child (age 12 and over): 2 dissolved capsules 4 times a day taken a half hour before meals and at bedtime.
Child (age 2-12): 1 dissolved capsule (100 mg) 4 times a day a half hour before meals and at bedtime. Dosage may be increased to about 13-18 mg per lb. of body weight in 4 equal doses.
Child (under age 2): about 10 mg per lb, of body weight a day divided into 4 equal doses. This product is recommended in infants
and young children only if absolutely necessary.
Eyedrops
Adult and Child (age 4 and over): 1-2 drops in each eye 4-6 times
a day at regular intervals. Overdosage
No action is necessary other than medical observation. Call your local poison control center or a hospital emergency room for more information. ALWAYS bring the prescription bottle or container.
Special Information
Cromolyn is taken to prevent or minimize severe allergic reactions. It is imperative that you take cromolyn products on a regular basis to provide equal protection throughout the day.
If you are taking cromolyn to prevent seasonal allergies, it is essential that you start taking the medication before you come into contact with the cause of the allergy and that you continue treatment while you are exposed to it.
Cromolyn oral capsules should be opened and their contents mixed with about 4 oz. of hot water. Stir until the powder completely dissolves and the solution is completely clear, then fill the rest of the glass with cold water. Drink the entire contents of the glass. Do not mix the solution with food, juice, or milk.
Do not wear soft contact lenses while using cromolyn eyedrops. The lenses may be replaced a few hours after you stop taking the drug. To prevent contamination, do not touch the applicator tip to any surface including the eyes or fingers.
Call your doctor if you develop wheezing, coughing, a severe drug reaction (see “Possible Side Effects”), rash, or any bothersome or persistent side effect.
Call your doctor if your symptoms do not improve or if they worsen.
If you forget to administer a dose, do so as soon as you remember and sqa(ZRMBmn-maining daily dosage evenly throughout ‘i!M day. Do not take a double dose.
Special Populations
PregnancylBreast-feeding. In animal studies, very large dosages of cromolyn administered by vein have affected the fetus, though no birth defects were reported. When this drug is considered crucial by your doctor, its potential benefits must be carefully weighed
against its risks.
It is not known if cromolyn passes into breast milk. Nursing
mothers who must use cromolyn should use infant formula. Seniors: Older adults with reduced kidney or liver function may require lower dosages.

Generic Name
Cyclobenzaprine (sye-cloe-BEN-zuh-prene) M
Brand Names Amrix
Type of Drug
Skeletal muscle relaxant.
Flexeril
Prescribed For
Serious muscle spasm and acute muscle pain; also used to treat fibrositis (muscular rheumatism).
General Information
Cyclobenzoprine hydrochloride is used to treat severe muscle spasms; it is prescribed as part of a coordinated program of rest, physical therapy, and other measures.
Cautions and Warnings
Do not take cyclobenzaprine if you are allergic or sensitive to any of its ingredients.
This drug should not be taken for several weeks following a heart attack or by people with abnormal heart rhythms, heart failure, heart block (disruption of the electrical impulses that control heart rate), or hyperthyroidism (overactive thyroid gland).
Cyclobenzaprine should be avoided by people with urinary retention, glaucoma, UC 1ntlreased eye pressure.
W)t arug may increase the chances of cavities or gum disease. Cyclobenzaprine is intended only for short-term use of 2-3 weeks.
Cyclobenzaprine is chemically similar to tricyclic antidepressants and may produce some of the more serious side effects associated with those drugs. Abruptly stopping cyclobenzaprine may cause nausea, headache, and feelings of ill health; this is not a sign of addiction.
Drug Interactions
•    The effects of alcohol, sedatives, or other nervous system depressants may be increased by cyclobenzaprine.
•    Cyclobenzaprine may increase some side effects of atropine, ipratropium, and other anticholinergic drugs.
•    The combination of cyclobenzaprine and a monoamine oxidase inhibitor antidepressant may produce very high fever, convulsions, and possibly death. Do not take these drugs within 14 days of each other.
•    Cyclobenzaprine may increase the effects of haloperidol, loxapine, molindone, pimozide, anticoagulant (blood-thinning) drugs, anticonvulsants, thyroid hormones, antithyroid drugs, phenothiazines, thioxanthenes, and nasal decongestants such as naphazoline, oxymetazoline, phenylephrine, and xylometazoline.
•    Barbiturates and carbamazepine may counteract the effects of cyclobenzaprine.
•    Fluoxetine, ranitidine, cimetidine, methylphenidate, estramustine, estrogens, and contraceptive drugs may increase the effects and side effects of cyclobenzaprine.
•    Cyclobenzaprine may counteract the effects of cto(\idine, guanadrel, and guanethidine.
Food Interactions  None known.
Usual Dose
Adult and Child (age 15 and over): 5-10 mg 3 times a day. Child (under age 15): not recommended.
above.    drowsiness, and dizziness.
le weakness. fatigue, nausea, consti-
ch, unpleasant taste, blurred vision,
ess, and confusion.
cts can occur in almost any part of the doctor if you experience any side ef- e.
Possible Side Effects
♦    Most common: dry
♦    Less common: muscl
upset stomach
nervousness, • Rare: Rare side effects
body. Contact your
fect not listed Overdosage
Cyclobenzaprine overdose may cause confusion, loss of con- centration, hallucinations, agitation, overactive reflexes, fever or vomiting, rigid muscles, and other side effects of the drug. It may also cause drowsiness, low body temperature, rapid or irregular heartbeat and other kinds of abnormal heart rhythms, heart failure, dilated pupils, convulsions, very low blood pressure, stupor, coma, and sweating. Overdose victims must be taken to a hospital emergency room. ALWAYS bring the prescription bottle or container.
Special Information
Cyclobenzaprine causes drowsiness, dizziness, or blurred vision in more than 40% of people who take it, which may interfere with the ability to perform complex tasks like driving or operating equipment. Avoid alcohol, sedatives, and other nervous system depressants because they can enhance sedative effects of cyclobenzaprine.
Call your doctor if you develop rash; hives; itching; urinary difficulties; clumsiness; confusion; depression; convulsions; difficulty breathing; irregular heart rate; chest pain; fever; yellowing of the skin or whites of the eyes; swelling of the face, lips, or tongue; or any other persistent or bothersome side effect.
If you forget a dose of cyclobenzaprine, take it as soon as you remember. If you take cyclobenzaprine once a day and it is almost time for your next dose, skip the one you forgot and continue with your regular schedule. If you take cyclobenzaprine twice a day and it is almost time for your next dose, take 1 dose as soon as you remember, another in 5 or 6 hours, and then go back to your regular schedule. If you take cyclobenzaprine 3 times a day and it is almost time for your next dose, take 1 dose as soon as you remember, another in 3 or 4 hours, and then go back to your regular schedule. Never take a double dose.
Special Populations
Pregnancy/Breast-feeding: -The safety of cyclobenzaprine in ‘jftg)T)1 women has not been established. Cyclobenzaprine should only be used if the potential benefits outweigh the risks.
It is not known if cyclobenzaprine passes into breast milk, but antidepressants with a similar chemical structure do pass into breast milk. Nursing mothers who must take this drug should consider using infant formula.
Seniors: Seniors are more likely to be sensitive to the effects of cyclobenzaprine. Use of Amrix in particular is not recommended
in the elderly.

Generic Name
Cyclosporine (sye-kim-SPQR-in)
Brand Names
Gengraf Neoral
Type of Drug  Immunosuppressant.
Restasis Ophthalmic Emulsion Sandimmune
Prescribed For
Kidney, heart, or liver transplantation; also used for bone-marrow, heart-lung, and pancreas transplants; also prescribed for patchy hair loss, rheumatoid arthritis, aplastic anemia, atopic dermatitis, Beh~et’s disease, cirrhosis of the liver, ulcerative colitis, dermatomyositis, eye symptoms of Graves’ disease, insulin-dependent diabetes, kidney inflammation, multiple sclerosis (MS), severe psoriasis and psoriasis-related arthritis, myasthenia gravis, pemphigus, sarcoidosis of the lung, and pyoderma gangrenosum. Cyclosporine eye emulsion is prescribed for dry eyes.
General Information
Cyclosporine is used to prevent rejection of transplanted organs. It works by blocking the activity of T-cells, which protect the body against invading microorganisms or foreign substances. Cyclosporine also prevents the production of a substance known as interieukin-11 that activates T-cells. In 1995, a new form of Cyclosporine called Neoral, a microemulsion, was introduced by its manufacturer. This form is as safe and effective as the original product but is better absorbed into the bloodstream and requires less medication to achieve the same effect. Cyclosporine eye emulsion treats dry eye caUV ,d by inflammation of the cornea and tissue kWA1 Covers the white part of the eye. It reduces inflammation and allows tears to form and flow.
Cautions and Warnings
Cyclosporine should be prescribed only by doctors experienced in immunosuppressive therapy and the care of organ-transplant patients. Sandimmune is always used with corticosteroid drugs like prednisone. Neoral and Gengraf have been used with a corticosteroid and azathioprine, an immune suppressant. When combined with other immune suppressants, cyclosporine must be used with great care because oversuppression of the immune system may lead to lymphoma or extreme susceptibility to infection.
Sandimmune, the original oral form of cyclosporine, is poorly absorbed into the bloodstream; it must be taken in a dosage that is 3 times greater than the injectable dosage. People taking this drug by mouth for a long period of time should have their blood checked for cyclosporine levels so that the dosage may be adjusted if necessary. Since more of both Gengraf and Neoral is absorbed into the blood you will probably need less of it. Do not substitute Neoral or Gengraf for Sandimmune; they are not equivalent to each other.
cyclosporine causes kidney toxicosis (kidney poisoning)—different from transplant rejection—in 25-35% of people taking it to prevent organ rejection. Mild symptoms usually start after about 2 or 3 months of treatment. Reducing drug dosage may control this effect. In one study, clonidine skin patches used before and after surgery decreased toxic risks to the kidney.
Liver toxicosis is seen in about 5% of transplant patients taking cyclosporine. It usually appears in the first month and may be controlled by reducing dosage.
Convulsions may develop, especially in people also taking high dosages of corticosteroids. Other nervous system side effects are listed below (see “Possible Side Effects”).
In one study, cyclosporine increased cholesterol and other blood-fat levels. It is not known how this affects people who take the drug on a long-term basis.
There is conflicting information on how cyclosporine affects blood sugar. Kidney-transplant patients taking the drug have developed insulin-dependent diabetes, which is related to the dosage of cyclosporine and reverses itself when you stop taking the drug. On the other hand, cyclosporine preserves the function of insuli(Nproducing cells in the pancreas and has allowed many insulin-dependent diabetics t0 11ve Without taking insulin.
UVb vaccines should not be given to people taking cyclosporine.
Do not use cyclosporine eye drops if you have an eye infection.
Small amounts of cyclosporine eye emulsion may be absorbed
into the bloodstream, but the risk of body-wide side effects is small.
Possible Side Effects
V Most common: Cyclosporine is known to be toxic to the kidneys. Your doctor will carefully monitor your kidney function while you are taking it. Other side effects are high blood pressure, increased hair growth, infection, and enlargement of the gums. Lymphoma may develop in people whose immune systems are excessively suppressed.
V Less common: tremors, cramps, acne, brittle hair or fingernails, convulsions, headache, confusion, diarrhea, nausea or vomiting, tingling in the hands or feet, facial flushing, reduced white-blood-cell and platelet counts, sinus inflammation, swollen and painful male breasts, drug allergy (symptoms include rash, itching, hives, and breathing difficulties), conjunctivitis (pinkeye), fluid retention and swelling, ringing or buzzing in the ears, hearing loss, high blood sugar, and muscle pain.
♦    Rare: blood in the urine, heart attack, itching, anxiety. depression, lethargy, weakness, mouth sores, difficulty swallowing, intestinal bleeding, constipation, pancreas inflammation, night sweats, chest pain, joint pain, visual disturbances, and weight loss. Contact your doctor if you experience any side effect not listed above.
Cyclosporine Eye Drops
♦    Most common: burning sensation.
✓    Less common: red-eye, discharge from the eye, overflow of tears, eye pain, a feeling of something in the eye, itching, stinging, and visual disturbances, usually blurring.
Drug Interactions
•    Cyclosporine should be used carefully with other kidney-toxic drugs including nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, naproxen, ac\d s0indac; ciprofloxacin; gentamicinjQtswnydin; vancomycin; trimethoprimsUM,M1~0oxazole; melphalan; amphotericin B; ketoconazole; azapropazon; colchicine; diclofenac; cimetidine; ranitidine; and tacrolimus.
•    Drugs that may increase blood levels of cyclosporine include contraceptive drugs; amiodarone; diltiazem; nicardipine; verapamil; fluconazole; itraconazole; ketoconazole; azithromycin; clarithromycin; erythromycin; quinapristin and dalfopristin; methylprednisolone—this combination also causes convulsions; allopurinol; bromocriptine; colchicine; imatinb-, danazol; and metoclopramide. With ketoconazole, your doctor may use this drug interaction to reduce your cyclosporine
dosage.
•    Drugs that decrease cyclosporine levels and may lead to organ rejection include octreotide, orlistat, sulfinpyrazone, ticlopidine, terbinafine, nafcillin, rifampin, carbamazepine, phenobarbital, phenytoin, and St. John’s wort. Rifabutin may also decrease concentrations of cyclosporine and should be used with caution.
•    Cyclosporine interferes with the body’s ability to clear digoxin, prednisolone, and statin drugs. People taking any of these drugs who start on cyclosporine must have their drug dosage reduced.
•    Combining cyclosporine and nifedipine may lead to gum overgrowth.
•    Cyclosporine increases blood potassium. Excessive blood-potassium levels may be reached if cyclosporine is taken with enalapril, lisinopril, a potassium-sparing diuretic such as spironolactone, salt substitutes, potassium supplements, or high potassium—low sodium—food.
•    Psoriasis patients using other immunosuppressant drugs or receiving radiation therapy should not take cyclosporine due to the danger of infection.
•    Cyclosporine prevents the normal body response to live vaccines. People taking cyclosporine should be vaccinated only after specific discussions with their doctors. You must wait for a period of several months to several years after stopping the medication before vaccination may be considered again.
Food Interactions
Cyclosporine may be taken with fMd 1111 upsets your stomach. For optimal QftlaWr~T)ess, avoid eating a fatty meal within half an hour of taking Neoral.
You may mix Neoral in a glass—not a paper or plastic cup—with room-temperature orange or apple juice or chocolate milk to make it taste better. Do not drink grapefruit juice because it speeds the breakdown of cyclosporine. Drink immediately after mixing, then put more juice or chocolate milk in the glass and drink it to be sure that the entire dose has been taken. Neoral should not be taken with unflavored milk because it may be unpalatable.
Usual Dose
In general, the usual dosage of Neoral is lower than Sandimmune, but dosage must be individualized for you by your doctor. Do not substitute one brand for the other.
Sandimmune
Adult: The usual oral dosage of cyclosporine is 6-8 mg per lb, of body weight a day. The first dose, typically 15 mg per lb., is given 4-12 hours before the transplant operation or immediately after surgery. This dosage is slowly reduced to 11-22 mg per lb. of body weight.
Child: Similar dosages are usually prescribed, but because children tend to release the drug from their bodies faster than adults, larger and more frequent doses may be needed.
Neoral and Gengraf
Adult: In newly transplanted patients, the usual oral dosage of Neoral is 3-4 mg per lb. of body weight a day divided into 2 doses. The initial oral dose of Gengraf is the same as for Sandimmune. The first dose is given 4-12 hours before the transplant operation or immediately after surgery. This dosage is continued after the operation for 1-2 weeks and then slowly reduced to maintain a target amount of cyclosporine in the body. Dosage may vary according to the organ transplanted.
In people being treated for rheumatoid arthritis or psoriasis, the initial dose of Neoral and Gengraf is 1.13 mg per lb. of body weight increased gradually to a maximum of 1.8 mg per lb. of body weight.
Child: Similar dosages are usually prescribed but, because children tend to release the drug from their bodies faster than adults, larger and more frequent doses may be needed.
cyclosporine Eye Emulsion
One drop in the affected eye(s) every Q hours. Before using, rotate and turn the vial Over a few times until you have a uniform, lft8, opaque fluid inside. If you use artificial tears, allow 15 minutes between products. Discard the open vial immediately after use.
Overdosage
Overdose victims may be expected to develop side effects and symptoms of extreme immunosuppression. Induce vomiting with ipecac syrup—available at any pharmacy—which is recommended up to 2 hours after the overdose was taken. Call your doctor or local poison control center before inducing vomiting. If you must go to a hospital emergency room, ALWAYS bring the prescription
bottle or container.
Special Information
Call your doctor at the first sign of fever; sore throat; tiredness’, weakness’, nervousness; unusual bleeding or bruising; tender or swollen gums; convulsions; irregular heartbeat; confusion; numbness or tingling of your hands, feet, or lips; breathing difficulties; severe stomach pain with nausea; or blood in the urine. Other side effects such as shaking or trembling of the hands, increased hair growth, acne, headache, leg cramps, nausea, or vomiting are less serious but should be brought to your doctor’s attention, particularly if they are bothersome or persistent.
Maintain good dental hygiene while taking cyclosporine and use extra care when brushing and flossing because the drug increases your risk of oral infection. cyclosporine may also cause swollen gums. See your dentist regularly.
Continue taking your medication as long as your doctor prescribes it. Do not stop taking it without your doctor’s knowledge. If you cannot take one of the oral forms, cyclosporine can be given by injection.
Do not keep either brand of the oral liquid in the refrigerator. After the bottle is opened, use the medication within 2 months. At temperatures below 68°F, Neoral can form a gel and a light sediment can form in Sandimmune. These do not affect the potency of either product. They can still be used and are effective.
If you forget a dose, take it as soon as you remember if it is within 12 hours of your regular dose. If not, skip the dose you forgot and continue with your regular schedule. Do not take a double dose.
For cyclosporine eye emulsion, each small plastic container is meant to be used once and then thrown away along with any remaining medication. Do not allow the tip of the disposable vial to touch 0Z QyE or any surface, as this may contaminate the emulsion.
Patients with decreased tear production typically should not wear contact lenses. But those that do must remove them before using cyclosporine eye emulsion. Lenses may be reinserted 15 minutes after using the medicine.
Special Populations
Pregnancy/Breast-feeding: In animal studies cyclosporine damages the fetus. Though a small number of pregnant women have taken cyclosporine without major problems, it is recommended that pregnant women avoid cyclosporine. When this drug is considered crucial by your doctor, its potential benefits must be carefully weighed against its risks.
cyclosporine passes into breast milk. Nursing mothers who must take cyclosporine should use infant formula.
Seniors: Due to decreased kidney function, seniors are more susceptible to kidney toxicosis.

Generic Name
Darunavir (dah-ROON-uh-vere)
Brand Name Prezista
Type of Drug  Protease inhibitor.
Prescribed For
Advanced human immunodeficiency virus (HIV) infection that has not responded to other protease inhibitors.
General Information
Part of the multidrug “cocktail” responsible for important gains in the fight against acquired immunodefiency syndrome (AIDS), darunavir is a member of a group of anti-HIV drugs called protease inhibitors. These drugs work at the end of the HIV reproduction process, whet) proteins are “cut” into strands of exactly tht VbYrect size to duplicate HIV. An enzyme known as protease cuts the protein. Protease inhibitors prevent the mature HIV virus from being formed by inhibiting this cutting process. Proteins that are cut to the wrong length or that remain uncut are inactive.
Darunavir must be taken with a low dose of ritonavir, another protease inhibitor, to extend the action of darunavir in the body.
Without ritonavii, darunavir would be eliminated too rapidly to be effective. Darunavir must also be accompanied by at least 2 other AIDS antivirals. Protease inhibitors revolutionized HIV treatment because, when taken in combination, they reduce the amount of HIV virus in the bloodstream to levels that are often undetectable by current methods—CD4 (immune system) cell counts and viral load (amount of virus in the blood) measurements. Multiple-drug therapy has transformed HIV from a fatal disease to a manageable chronic illness.
Cautions and Warnings
Do not take darunavir if you are allergic or sensitive to any of its ingredients, to sulfa drugs, or to ritonavir.
Darunavir can cause a severe or life-threatening rash.
If a serious toxic reaction occurs while taking darunavir, you should stop the drug until your doctor can determine the cause or until the reaction resolves itself. Then treatment can be resumed.
This drug is primarly broken down in the liver. Use caution if you have moderate to severe liver disease.
Darunavir may raise your blood sugar, worsen your diabetes, or bring out latent diabetes. People with diabetes who take darunavir may need the dosage of their antidiabetes medication adjusted.
People with hemophilia may be more likely to bleed while taking a protease inhibitor.
The HIV virus may become resistant to darunavir or other protease inhibitors. For this reason it is essential that you take darunavir exactly according to your doctor’s directions.
Protease inhibitors can cause body fat redistribution, including increased fat deposits in the upper back and neck, breast and around the back, chest, and stomach. Fat may be lost from the legs, arms, and face. Some people with HIV and a history of an opportunistic infection may develop signs and symptoms of the infection soon after anti-HIV treatment is started. This is called immune reconstitution syndrome.
Darunavir is involved in many drug interactions. Check with your doctor before adding angt ng new to your treatment program.
Possible Side Effects
V Most common: diarrhea, nausea, headache, and common cold symptoms.
of constipation.
Drug Interactions
•    Do not take any of the following medicines with darunavir + ritonavir: astemizole, terfenidine, ergot-based drugs for migraine headache, cisapride, pimozide, midazolam, or triazolam. Mixing these drugs with darunavir + ritonavir can result in very high blood levels and serious side effects.
•    Carbamazepine, phenobarbital, phenytoin, rifampin, and St. John’s wort can substantially reduce blood levels of darunavir. Do not mix these medicines.
•    Lopinavir + ritonavir and saquinavir can significantly reduce blood levels of darunavir. Darunavir significantly increases blood levels of lopinavir + ritonavir. Do not mix these drugs.
•    Mixing darunavir with indinavir can increase blood levels of both drugs.
•    Darunavir + ritonavir does not appear to affect blood levels of atazanavir, nor does atazanavir appear to affect blood levels of darunavir + ritonavir. It may be possible to combine these two protease inhibitors.
•    Taking darunavir with tenofovir can increase blood levels of both drugs. These drugs can be combined with no dose adjustments, though it is necessary to watch carefully for kidney damage related to tenofovir.
•    Darunavir can increase blood levels of efavirenz and efavirenz reduces darunavir levels. These medicines should be mixed with caution.
•    Darunavir increases nevirapine blood levels but the raMUNnation can be taken with no dose a-Syoslment.
•    If didanosine (SWpat 01 a darunavir + ritonavir treatment pro~ram, it must be taken on an empty stomach, 1 hour before or 2 hours after darunavir + ritonavir, which should be taken with food.
•    Darunavir increases blood levels of clarithromycin, itraconazole, and ketoconazole. Daily dosage of itraconazole and ketoconazole should not exceed 200 mg. No clarithromycin
Possible Side Effects (continued)
♦    Less common:    abdominalinal pain, and
♦    Rare: Rare side effects can occur in almost any part
body. Contact your doctor if you
ou experience any side ef
fect not listed above.
adjustment is necessary in people with normal kidney function.    the Darunavir + ritonavir may reduce vonconazole levels in t e
blood. Do not mix these medicines.
•    Darunavir + ritonavir can increase rifabutin levels in the blood-
stream. Rifabutin can also reduce darunavir levels in the
bloodstream. If rifabutin is mixed with darunavir + ritonavir,
the rifabutin dose should be 150 mg every other day.
•    Caution should be exercised when combining darunavir + ritonavir with calcium channel blockers such as felodipine, nifedipine, and nicardipine.
•    Darunavir increases blood levels of the heart antiarrhythmic drugs bepridil, lidocaine, and quinidine. These drugs should be used together with caution and only in situations where blood levels of the heart drugs can be monitored regularly.
•    Darunavir + ritonavir can reduce blood levels of warfarin. It is necessary to monitor warfarin levels while taking this combination.
•    Darunavir + ritonavir can raise blood levels of the tricyclic antidepressant desipramine and the tetracyclic antidepressant trazodone. Dosage reduction is recommended.
•    Darunavir + ritonavir may reduce blood levels of the SSRI antidepressants sertraline and paroxetine. SSRI doses may have to be increased to account for this effect.
•    Darunavir + ritonavir can drastically increase the blood levels of some statin-type cholesterol-lowering drugs, substantially increasing the risk of statin side effects. Simvastatin, pravastatin, and lovastatin should not be mixed with darunavir + ritonavir. It is also possible to take darunavir + ritonavir with atorvastatin, although it can increase the level of atorvastatin in the bloodstream. If atorvastatin is prescribed, it is best to begin with 10 mg a day and slowly increase the dose as necessary. Little is known about how darunavir + ritonavir affects rosuvastatin. The safest statin to take with darunavir + ritonavir is fluvastak”.
•    Darunavir + ritonaxk Can increase blood levels of inhaled MT lCosteroids dexamethasone and fluticasone, the anti-rejection drugs cyclosporine, tacrolimus, and sirolimus. The corticosteroids reduce darunavir blood levels, interfering with its effectiveness.
•    Darunavir + ritonavir can reduce methadone levels in the bloodstream. Methadone dose adjustment may be needed.
•    Darunavir + ritonavir reduces the effectiveness of some contraceptive drugs by decreasing the amount of the hormones ethinyl estradiol and norethindrone in the bloodstream. Women mixing these medicines should use additional contraceptive measures (e.g., condoms).
•    Protease inhibitors may drastically increase blood levels of erectile dysfunction drugs sildenafil, vardenafil, and tadalafil, increasing the risk of side effects including low blood pressure, visual changes, and persistent, painful erection.
•    Dexamethasone may reduce blood levels of darunavir.
Food Interactions
Take darunavir with food. The amount of darunavir absorbed into the blood is vastly reduced when it is taken on an empty stomach, thus negating its antiviral effects.
Usual Dose
Adult: 600 mg (2 300-mg tablets) with 1 00 mg ritonavir twice a day. Do not chew these tablets.
Child: not recommended.
Overdosage
Little is known about the effects of darunavir overdose, but 3200 mg of darunavir has been given to study volunteers with no adverse effects. Call your local poison center or hospital emergency room for more information. If you take the victim to a hospital emergency room, ALWAYS bring the prescription bottle or container.
Special Information
Darunavir is not a cure for HIV. It will not prevent you from transmitting the HIV virus to another person; you must still practice safe sex. You may still develop opportunistic infections or other complications associated with advanced HIV disease.
The long-term effects of this drug are not known.
It is imperative for you to take this medication exactly according to your doctor’s instructions. Do not skip any doses. Skipping doses of darunavir increases the risk that you will become resistant k,3 ft drug. If you forget a dose of darunavir or ritonavir and remember within 6 hours, take it as soon as you remember and then continue with your regular schedule. If 6 hours have passed since the time when you should have taken your medicine, skip the forgotten dose and take your next dose at the regular time. Do not take a double dose.
Special populations
Pregnancy/Breast-feeding: Animal studies with darunavir reveal no damage to the fetus, but there are no data on how this drug affects pregnant women. Darunavir should only be used during pregnancy after carefully weighing its potential benefits against its risks.
It is not known if darunavir passes into breast milk. Nursing mothers with HIV should use infant formula, regardless of whether they take this drug, to avoid transmitting the virus.
Seniors: Seniors can take this drug without special precaution.

Various Anti-Allergy Drugs

Tuesday, May 19th, 2009

Various anti-allergy drugs
An allergic reaction is a lengthy, complex process, and the various anti-allergy drugs all work on different stages of that process. That is why it often makes sense to use several different drugs for the same allergic condition: they each tackle the problem in their own way.
Steroids (see p. 140) intervene at a very late stage, quelling the inflammation that follows on from an allergic reaction. Using a steroid is rather like calling the fire brigade to put out a fire, whereas using an antihistamine (see p. 138) is like having fire-proof doors, to prevent the fire spreading at an early stage. Cromoglycate-type drugs (see below) intervene at an even earlier stage. They are like basic fire prevention - teaching children not to play with matches, or fitting smoke detectors.
Anti - leukotnene drugs (see p. 149) work at roughly the same stage of the process as anti-histamines but tackle an entirely different aspect of the allergic reaction.
Cromoglycate-type drugs
These drugs are also referred to as mast-cell stabilisers or mast-cell Mockers.
There are three drugs in this group, sodium cromoglycate (also spelled cromoglicate), nedocromil sodium, and lodoxamide. All operate at an early stage of the allergic reaction, stopping it before it actually starts. They stabilise the outer membrane of the mast cells (see box on p. 12), which prevents the allergic response from occurring.
Some common brand names
Common brand names of cromoglycate-type drugs include:
inhalers - Cromogen Easi-Breathe, Intal, Tilade
eye drops - Hay-Crom, Opticrom, Rapitil, Vividrin, Viz-on nose sprays - Rynacrom, Vividrin
capsules - Nalcrom
This is a far more satisfactory way of dealing with an allergic reaction than trying to tackle it after the reaction has occurred. But from a purely practical point of view, it has a drawback. I order to work at all, these drugs must reach the mast cells in advance of the allergen. They are of very little use if taken after the allergic reaction has begun.
For those who are taking cromoglycate-type drugs on a regular schedule, several times a day, it is very important to be conscientious about taking them on time. This maintains the protective effect of the drug, without any gaps.
If you are using these drugs on an ‘as-needed’ basis, you should take them 30 minutes before an allergen is encountered. or 30 minutes before a bout of exercise, if they are being prescribed for exercise-induced asthma. (Note that children sometimes respond differently, getting protection from these drugs immediately.)
The effect of these drugs takes time to build up. You should take them regularly for at least four weeks before deciding whether they are helping you or not.
One point in favour of cromoglycate-type drugs is that they are extremely safe, with few or no side effects in most people. Sadly, they do not work for everyone. A fairly high percentage of children respond well to them, but the response rate is much lower for adults. Nevertheless, adult allergy sufferers, especially those who need steroids to control their symptoms, should always be given the opportunity to try out these drugs. When cromoglycate-type drugs do work, they are very effective and almost always trouble-free, so they are a good alternative to steroids.
Both sodium cromoglycate and nedocromil sodium are available in inhaler form for asthma (see p. 157). Sodium cromoglycate is also available as nose drops for hayfever and other nasal allergies.
All three drugs are available as eye drops. Recent evidence suggests that sodium cromoglycate drops are less effective than the other two, particularly for the treatment of severe allergic conjunctivitis (inflammation of the eye).
Sodium cromoglycate is available in capsule form for food allergy. Note that these capsules are of very limited value in food allergy, and are certainly not a substitute for food avoidance. They do reduce sensitivity a little and can sometimes be helpful for those with multiple food allergies (see p. 67).
Side effects
There are no serious side effects at all for nedocromil sodium. cromoglycate can, very rarely, cause joint pain and swelling. An allergic reaction to the drug itself is even more uncommon. Stop taking the drug and see your doctor promptly if either of these occurs.
The only other side effects that have occasionally been reported are headache, nausea and vomiting. None of these indicates any damaging effect by the drugs – they are all minor side effects.
Eye drops containing these drugs may cause stinging and burning when inserted, but this is a minor side effect and usually wears off. Flushing and dizziness have sometimes been reported with lodoxamide eye drops.
Nose drops may also cause local irritation. This could be due to the drug itself, in which case it is a minor side effect. Alternatively, the irritation may be due to the preservative used or some other non-drug ingredient (see box on p. 33).
Occasionally cromoglycate nose drops cause bronchospasm – contraction of the airway muscles – but this tends to wear off quite quickly. Bronchospasm can also occur when cromoglycate-type drugs are inhaled (see p. 157).
Anti - leu kotriene drugs
These drugs, which have a set of very specific effects (see p. 159), were originally designed to treat asthma. Their potential for treating other allergic diseases is currently being explored:
•    Several studies show that they work well for perennial allergic rhinitis brought on by allergens such as house-dust mite. They also have some effect on hayfever, but standard treatment (such as antihistamines plus a steroid spray for the nose) is more effective.
•    They are especially useful for both rhinitis and asthma in patients suffering from triad (see box on p. 28). Research shows that they also reduce asthmatic reactions to very small test doses of aspirin, but they don’t give protection against anaphylaxis brought on by normal doses.
•    They have also been used successfully in cases of chronic urticaria and for some patients with delayed pressure urticaria. It seems plausible that they would also be helpful for chronic urticarla linked to aspirin sensitivity.
•    Preliminary trials suggest that these drugs might be useful in atopic eczema. Some studies show a very good response that allows a reduction in steroid creams.
•    Montelukast works very well for eosinophilic gastroenteritis and eosinophilic oesophagitis (see p. 72), according to some new studies.
For side effects of these drugs see pp. 159-60.
Anti-IgE drugs
Since the antibody IgE (see box on p. 12) is such a crucial player in allergic reactions, developing drugs that disable this antibody should help allergy sufferers. The first such drug is omalizumab (brand name Xolair) which was licensed for use in the United States in 2003. It is expected to become available in Britain some time in the next few years.
Omalizumab binds to IgE antibodies and stops them from interacting with mast cells, so blocking any allergic reaction. The drug is given as a ‘depot injection’, just under the skin, every 2-4 weeks. It is gradually released from the injection site and moves around the body in the blood, mopping up IgE molecules.
At present, omalizumab is used for severe hayfever and for people with asthma who are not responding well to the usual treatments. It is only worth using if there is clear evidence that allergies play a part in the asthma. Patients who use omalizumab are often able to reduce their dose of inhaled steroids – and they suffer fewer serious asthma attacks and have better lung function. Some patients can even stop using steroids completely.
Other anti-IgE drugs are in the pipeline. Pilot studies show that one works very well for peanut allergy: after just four injections, sensitivity to the allergen falls sharply, reducing the risk of anaphylaxis from traces of peanut eaten accidentally.
More powerful anti-allergy drugs
Occasionally people with severe allergies, who are on constant high doses of steroid tablets, or who fail to respond to steroids, need treatment with powerful anti-inflammatory drugs, such as methotrexate or cyclosporin. These suppress the immune system, and extremely careful monitoring for side effects is needed.
Adrenaline (epinephrine)
Anyone who has suffered anaphylactic shock (see p. 58) should be carrying a special syringe, called an auto-injector, loaded with adrenaline. The injector is very simple to operate and is designed for emergencies. Most allergy sufferers, even children, can give themselves the injection – or a parent or other adult can give it.
Some asthmatics, and those with food allergy who suffer swelling of the throat, may be given adrenaline in inhaler form as well (see pp. 155-6). This can be useful as an additional treatment but it’s definitely not a substitute for an injector.
See pp. 98-9 for instructions on using adrenaline in a crisis.
Wherever you go, take your injector with you. Always keep it close at hand: you need to be able to use it within minutes of the allergic reaction starting. You may be unable to speak (and therefore unable to ask someone else to fetch it) quite soon after the attack begins. The injector must never be refrigerated. It can also be damaged by sunlight and excess heat.
If you live in the countryside or in an area with a poor ambulance sevice, or if you are going camping or hiking somewhere remote, ask your doctor for a second injector, or one that can deliver multiple injections. Also ask about the maximum number of injections that can be given, and never exceed this total. Some doctors believe everyone should have two injectors, just in case the first dose doesn’t do the trick and help is slow in coming.
It is vital that you are shown exactly how to use the auto-injector. Canadian researchers discovered that only one in four
Some common brand names
Common brand names of adrenaline preparations include: auto-injectors – Anapen, EpiPen
inhalers – AsthmaHaler Mist, Bronkaid, Epiphrine
health professionals got the technique correct when demonstrating how to use an auto-injector In this study, pharmacists were much the best as regards accurate instructions. Dummy injectors are useful for training purposes and most pharmacies have them.
When the adrenaline auto-injectors expire, they can be very useful for practising with, or for showing a new baby-sitter or teacher – practise on an orange or grapefruit.
If you are taking beta-blockers (e.g. for a heart condition or anxiety), adrenaline may not have much effect.
Heavy daily use of beta-2 relievers for asthma (see p. 152) will also make adrenaline less effective when you need it.
Side effects
The important side effects of adrenaline involve the heart. Anyone with a heart condition should be given special advice in advance by their doctor about using adrenaline. The same goes for people with diabetes, hyperthyroidism or high blood pressure, and anyone taking tricyclic anti-depressants. There are quite a few minor side effects from adrenaline, such as anxiety, trembling, nausea. sweating, dizziness and cold extremities. These soon wear off.
Drugs that can make you worse
Aspirin and its relatives have a very bad effect on some people with rhinitis and/or asthma (see box on p. 151). Unfortunately, recent research shows that paracetamol is not safe either. It makes asthma more likely to develop in those who do not yet have the disease, and increases the severity of asthma symptoms for those who do. Unlike aspirin, paracetamol affects everyone, because it lowers the levels of a natural antioxidant, called glutathione, which the body makes to protect the lungs from oxidants. The greatest effects are seen in people who take paracetamol regularly (once a week or more), but even an occasional dose makes some difference.
All the other drugs that can make you worse are prescription drugs, and your doctor should be alert to the dangers. But doctors are overworked and sometimes forget, so it is sensible to know about the risks for yourself. If you have any doubt about the drugs you are taking, ask a pharmacist.
Beta-blockers are a major hazard for people with allergies. They can make the airways contract, and can bring on a serious asthma attack. They also make anaphylaxis more likely in someone who already has allergic reactions (see p. 59) and they increase the risk of a severe reaction to
immunotherapy (see p. 166) or skin-prick tests (see p. 91). Beta-blockers are prescribed for high blood pressure, angina and other heart problems, migraine and thyroid disease. There are alternative drugs in all cases. Sometimes asthma develops in people who have been taking beta-blockers for years. The beta-blockers are not responsible for this, but once asthma has begun, they will make symptoms worse. Eye drops for the treatment of glaucoma may also contain beta-blockers and can have a bad effect on asthmatics.
ACE inhibitors, used for heart conditions, may cause a cough and airway narrowing. They may also increase the risk of a severe reaction to immunotherapy.
Female hormones affect asthmatics, so taking the contraceptive pill or hormone replacement therapy (HRT) may make asthma worse. Progesterone-only contraceptive pills tend to cause fewer problems.
The drug isoniazid (INH), prescribed for tuberculosis, makes the body far more susceptible to histamine in foods (see p. 200).
An allergic reaction to a specific drug (e.g. penicillin) can also occur in some people, resulting in urticaria, or even anaphylactic shock.
Aspirin sensitivity
Aspirin sensitivity is not an allergic reaction, because neither IgE nor mast cells are involved. What causes this problem is a metabolic abnormality — a malfunction in one aspect of the body’s chemistry. The details of this are very complicated: you may want to skip the next three paragraphs and
simply read about how to cope with the problem.
The exact nature of aspirin sensitivity is still far from clear, but it seems to involve a relatively poor production of prostaglandins, combined with a plentiful production of leukotrienes. Both these substances are messenger chemicals which, broadly speaking, promote inflammation. But the details of their pro-inflammatory activities differ. It seems that, ideally, the body should have a harmonious balance between the two, and an imbalance produces problems.
Both prostaglandins and leukotrienes are manufactured from certain fats that are found in the diet. These fats, the raw materials, are worked on initially by two different enzymes — one that leads to the production of prostaglandins and another that leads to the production of leukotrienes.
If one of these enzymes is defective, it may mean that the other is oversupplied with raw materials, resulting in a serious imbalance between prostaglandins and leukotrienes. In those with aspirin sensitivity, or at risk of developing aspirin sensitivity, the enzyme that produces prostaglandins seems to be defective.
Even in the absence of aspirin, this imbalance in the production of prostaglandins and leukotrienes causes problems. It leads to symptoms such as chronic urticaria (see p. 51) or rhinitis, nasal polyps and asthma (a cluster of symptoms that is commonly called triad — see box on p. 28).
Taking aspirin can make the imbalance between prostaglandins and leukotrienes even worse in a person with this underlying abnormality. Aspirin exerts its painkilling effects by disabling the main prostaglandin-making enzyme — the enzyme that is already defective.
When someone with aspirin sensitivity takes aspirin, they may suffer worsening asthma, a severe asthma attack or — the worst-case scenario —collapse. This is a potentially fatal reaction, similar to anaphylaxis, requiring emergency medical treatment (see p. 101).
The greatest puzzle about aspirin sensitivity is why it often takes so long to develop in someone who already has the symptoms of triad —indicating the basic metabolic abnormality. It may be as much as 20 years from when someone has their first triad symptoms to when they begin reacting badly to aspirin.
If you have triad symptoms already, but no aspirin sensitivity yet, what should you do? Unfortunately, there are no safe tests for aspirin sensitivity at present — taking a small dose of aspirin and seeing what happens is very hazardous. It is probably best to assume that you are going to become sensitive to aspirin at some stage, and avoid all aspirin and aspirin-like drugs. Caution is the best plan here because aspirin sensitivity can come on very suddenly, and be life-threatening the very first time it occurs. Note
that some triad sufferers have polyps and rhinitis but no asthma until they actually develop aspirin sensitivity — a dose of aspirin suddenly brings on their first asthma attack plus other symptoms of aspirin sensitivity.
Avoiding aspirin itself is not difficult, but aspirin-like drugs pose more of a problem. Every year there are a number of deaths from these drugs. Some cases occur because a busy doctor momentarily forgets that a patient should not take these drugs. The drugs that need to be avoided are all known as non-steroidal anti-inflammatory drugs (NSAIDs), COX-1 inhibitors or COX-2 inhibitors. However you will not see any of these names on the packet. These drugs are very widely used for pain relief (e.g. in headache and backache remedies such as Nurofen), for the treatment of arthritis, and for several other inflammatory diseases.
There are dozens of non-steroidal anti-inflammatory drugs available, and many are sold under several different brand names. The list grows every year, as new drugs or new brands are launched. The only way to avoid these drugs is to be very cautious:
•    When buying any cold- or flu-remedies, painkillers, medicines for sprains or sports injuries (including those you apply directly to the skin), headache tablets or migraine tablets, always buy them at a chemist’s shop rather than a supermarket, and check with the pharmacist that they do not contain aspirin or aspirin-like drugs.
•    Be cautious also about remedies for an upset stomach. A few (e.g. Alka-Seltzer) contain aspirin.
•    Don’t take any drugs unless you are 100% sure of what they contain. Remember that the ingredients of a familiar brand name can sometimes change — read the label every time.
•    When a doctor prescribes any new drug, always mention that you are sensitive to aspirin, or that you have triad symptoms. Alternatively, check with the pharmacist when the prescription is filled.
•    Aspirin-free painkillers almost always contain paracetamol, a drug which can cause a severe reaction (similar to the collapse induced by aspirin itself) in about 5% of those with aspirin sensitivity. If you are taking paracetamol for the first time, start with half a tablet. Be sure that, for the next 2-3 hours, you have a way of getting to hospital quickly should you start to feel ill. (Note that paracetamol has another entirely separate effect, increasing the severity of asthma, and it is best not to take it too often — see box on p. 150.)
Avoiding all aspirin-like drugs will prevent you having anaphylaxis or severe attacks of asthma. Unfortunately, triad symptoms will not go away however careful you are about avoiding aspirin.
It is well worth trying the new anti-leukotriene drugs (see p. 149), especially if you have aspirin-induced asthma. They seem to help with triad symptoms by curtailing the activities of leukotrienes and so redressing the balance between leukotrienes and prostaglandins.