Aug
1
Cholestyramine
August 1, 2009 | Leave a Comment
Generic Name
Cholestyramine (kol-es-TYE-rah-meen) 0
Brand Names
LoCHOLEST Questran
LoCHOLEST Light Questran Light Prevalite
The information in this profile also applies to the following drugs:
Generic Ingredient: Colesevelam Hydrochloride WelChol
Generic Ingredient: Colestipol Hydrochloride Colestid
Type of Drug
Anti -hyperli pidemic (blood-fat reducer).
Prescribed For
High blood-cholesterol levels; generalized itching associated with bile duct obstruction—cholestyramine only; colitis; digitalis or thyroid overdose; and pesticide poisoning.
General Information
Cholestyramine resin lowers blood-cholesterol levels by absorbing bile acids in the bowel. Since the body uses cholesterol to make the bile acids—needed to digest fat—fat digestion can only continue by making more bile acid from blood cholesterol. This results in lower blood-cholesterol levels 4-7 days after starting cholestyramine.
Cholestyramine w3Cks entirely Within the bowel and is never absorbed into the bloodstream. Though usually given 3-4 times a day, there appears to be no advantage to taking it more often than twice a day. The cholesterol-lowering effect of cholestyramine may be increased when it is taken with an HMG-CoA inhibitor or nicotinic acid. In some kinds of hyperlipidemia, colestipol may be more effective in lowering total blood cholesterol than clofibrate.
Cautions and Warnings
Do not use cholestyramine if you are allergic or sensitive to any of its ingredients or if your bile duct is blocked. The powder form should not be taken dry; doing so may result in the inhalation of powder into your lungs or a clogged esophagus.
If you are being treated for hypothyroidism, diabetes, kidney or blood vessel disorder, obstructive liver disease, or alcholism, consult your doctor before taking cholestyramine.
Cholestyramine may cause or worsen constipation and hemorrhoids. Most constipation is mild, but some people may need to stop the medication or take less of it.
Possible Side Effects
✓ Most common: constipation, which may be severe and in rare cases result in bowel impaction. Hemorrhoids may be worsened.
♦ Less common: abdominal pain and bloating, and bleeding disorders or black-and-blue marks due to interference with the absorption of vitamin K, a necessary factor in the blood clotting process. One person developed night-blindness because the medication interfered with vitamin A absorption into the blood. Other side effects include belching, gas, nausea, vomiting, diarrhea, heartburn, and appetite loss. Your stool may have an unusual appearance because of a high fat level.
✓ Rare: Rare side effects can affect your mouth, stomach and intestines, muscles and joints, mental status, urinary tract, and breathing. Contact your doctor if you experience any side effect not listed above.
Drug Interactions
O Cholestyramine interferes with the absorption of virtually all oral drugs, including acetaminophen, amiodarone, aspirin, cephalexin, chenodiol, clindamycin, clofibrate, contraceptive drugs, corticosteroids, diclofenac, iopanoic acid, iron, digitalis drugs, furosemide, gemfibrozil, glipizide, hydrocortisone, imipramine (an antidepressant), methyldopa, mycophenolate, nicotinic acid, penicillin, phenobarbital, phenytoin, piroxicam, propranolol, tetracycline, thiazide diuretics, thyroid drugs, tolbutamide, trimethoprim, ursodiol, warfarin and other anticoagulant (blood-thinning) drugs, and vitamins A, D, E, and K. Take other medications at least 1 hour before or 4-6 hours after taking cholestyramine.
Food Interactions
Take this medication before meals. The powder may be mixed with soda, water, juice, cereal, or pulpy fruits, such as applesauce or crushed pineapple. Cholestyramine bars should be thoroughly chewed and taken with plenty of fluids. Colestipol pills are swallowed whole.
Usual Dose
Cholestyramine: 4 g (1 packet) or 1 level scoopful taken 1-2 times a day or up to 6 times a day.
Colesevelam: 6 tablets once a day or in 2 divided doses. Colestipol: 2-16 g (1-6 packets) once a day or in divided doses.
Overdosage
The most severe effect of overdose is obstruction of the gastrointestinal tract. Take the overdose victim to a hospital emergency room. ALWAYS bring the prescription bottle or container.
Special Information
Do not swallow the granules or powder in their dry form. Prepare each packet of powder by mixing it with soup, cereal, or pulpy fruit or by adding the powder to a 6-oz. glass of liquid, such as a carbonated beverage. If some of the drug sticks to the sides of the glass, rinse it with liquid and drink the remainder.
Constipation, gas, nausea, and heartburn may occur and then disappear with continued use of this medication. If constipation is a problem, your doctor may recommend drinking more fluids and taking a fiber supplement. Call your doctor if these side effects persist or if you develop unusual problems such as bleeding from the gums or rectum.
If you miss a dose of cholestyramine, skip it and continue with your regular scheduke. Do not take a double dose.
Special Populations
Pregnancy/Breast-feeding: While cholestyramine does not affect the fetus directly, it may prevent the absorption of vitamins A, D, and E and other nutrients essential to the fetus’ proper development–even when you take, a prenatal vitamin supplement.
When this drug is considered crucial by your doctor, its potential benefits must be carefully weighed against its risks.
Cholestyramine is not absorbed into the body. However, reduced absorption of vitamins A, D, and E and other nutrients may make your milk less nutritious. Nursing mothers who must take cholestyramine should use infant formula.
Seniors: Seniors are more likely to experience side effects, especially those relating to the bowel.
Jul
16
Aldosterone Blockers
July 16, 2009 | Leave a Comment
Type of Drug
Aldosterone Blockers (al-DOH-stir-own)
Brand Names
Generic Ingredient: Eplerenone Inspra
Generic Ingredient. Spironolactone Aldactone
Combination Product
Generic Ingredients: Hydrochlorothiazide + Spironolactone Aldactazide
Prescribed For
High blood pressure, cirrhosis, and congestive heart failure (CHF); also used for people with low blood potassium who require a diuretic.
General Information
Aldosterone blockers limit the access of aldosterone—a hormone that helps to regulate several different body functions—from its receptor. Too much aldosterone results in high sodium levels, which can lead to water retention and potassium loss; it can also affect the size, shape, and function of the heart. Aldosterone blockers are generally combined with other medicines in the management of disease. These drugs are useful in removing excess body fluids in conditions associated with high aldosterone levels.
One in every ten people with high blood pressure has excess aldosterone in their systems. In people with congestive heart failure (CHF), aldosterone levels can be 20 times higher than normal, which can worsen their condition, making the use of aldosterone blockers an important part of their treatment. Aldosterone block-ers also help the heart return to normal size, shape, and function in people with heart failure. Eplerenone is broken down in the liver, primarily by an enzyme system known as CYP3A4.
Cautions and Warnings
Do not take aldosterone blockers if you are allergic or sensitive to any of their ingredients.
Do not use aldosterone blockers if you have kidney failure or high blood potassium.
People with liver disease should be cautious about using a!- dosterone blockers.
People taking an aldosterone blocker should have their potassium levels checked periodically.
People with diabetes who have albumin in their urine should not take aldosterone blockers.
Possible Side Effects
Eplerenone
✓ Less common: dizziness, diarrhea, fatigue, flu-like symptoms, coughing, abdominal pain, elevation of blood cholesterol and/or triglyceride levels, elevation of blood potassium levels, and albumin in the urine.
✓ Rare: enlargement of the breasts in males, irregular menstrual cycles in women, and painful breasts. Contact your doctor if you experience any side effect not listed above.
Spironolactone
✓ Less common: drowsiness, lethargy, headache, gastrointestinal upset, cramps and diarrhea, rash, mental confusion, fever, feeling unwell, enlargement of the breasts in males, impotence, and irregular menstrual cycles or deepening of the voice in women.
Drug Interactions
• Do not combine eplerenone with itraconazole or ketoconazole. These drugs can cause the amount of eplerenone in the blood to increase by up to 500% and may cause fatal increases in blood potassium.
• Mixing eplerenone with erythromycin, fluconazole, saquinavir, or verapamil increases the amount of eplerenone in the blood. People taking this combination must watch for signs of high blood potassium (see “Special Information”) and have their blood potassium levels checked regularly.
• Combining a potassium supplement and an aldosterone blocker can lead to dangerously high blood levels of potassium. Do not use a salt-substitute or take any extra potassium unless prescribed by your doctor.
• Combining an aldosterone blocker with an ACE inhibitor or an angiotensin H receptor blocker (ARB) may significantly raise blood potassium. Be sure your doctor monitors your potassium levels if you combine these drugs.
• Spironolactone may interfere with anticoagulant (blood-thinning) drugs and mitotane (an anticancer drug).
• Aspirin can interfere with the diuretic effect of spironolactone but does not alter its effect on high blood pressure or CHF.
• Combining spironolactone with alcohol, barbiturates, or narcotics can lead to dizziness or fainting when rising suddenly from a sitting or lying position.
• Combining spironolactone and a corticosteroid can lead to very low blood potassium.
• Spironolactone may alter your response to drugs used during general anesthesia.
• Lithium generally should not be combined with any diuretic.
• Combining nonsteroidal anti-inflammatory drugs (NSAIDs) with aldosterone blockers can lead to severe elevations of blood potassium and reduce the blood-pressure-lowering effect of the diuretic.
• Spironolactone may raise digoxin blood levels and increase the risk of severe digoxin side effects. Your doctor may have to adjust your digoxin dosage.
• St. John’s wort (a CYP3A4 inducer) may decrease eplerenone levels by about 30%.
Food Interactions
Food appears to increase the amount of spironolactone absorbed into the blood. Take this drug with food at the same time every day. Eplerenone may be taken without regard to food or meals. Taking this drug with grapefruit juice increases the amount of drug absorbed into your body.
Usual Dose
Eplerenone
Adult 50-100 mg a day. Child: not recommended.
Spironolactone
Adult: Starting dosage is 50-100 mg a day in divided doses for high blood pressure; 25-200 mg a day in divided doses for high fluid levels related to other diseases; and 25-100 mg a day for low potassium levels related to diuretic use.
Child: 1-2 mg per lb. of body weight a day.
Spironolactone + Hydrochlorothiazide Adult: 1-4 tablets daily.
Overdosage
Eplerencne overdose may lead to low blood pressure and high blood potassium. Spironolactone overdose may lead to drowsiness. confusion, rash, nausea, vomiting, dizziness, and diarrhea. Rarely. coma may occur in people with severe liver disease. High blood potassium may also occur, especially in people with kidney zsease. Call your local poison control center or a hospital emercency room for more information. If you seek treatment, ALWAYS oring the prescription bottle or container.
Special Information
<e a c!osterone blockers exactly as they are prescribed.
High blood levels of potassium associated with aldosterone blockers may cause weakness, lethargy, drowsiness, muscle pain or cramps, and muscular fatigue. Use caution while doing anything that requires intense concentration, like driving or operating machinery.
Do not use a salt substitute or take anything else that is a source of extra potassium, including many multivitamin or supplement products.
People with high blood pressure should not self-medicate with over-the-counter cough, cold, or allergy remedies containing stimulants. These drugs can raise blood pressure effectiveness and have an adverse effect on the heart.
!f you forget a dose, take it as soon as you remember. If it is almost time for your next dose, skip the one you forgot and continue with your regular schedule. Do not take a double dose.
Special Populations
Pregnancy/Breast-feeding: Animal studies with eplerenone showed no effects on a developing fetus. Spironolactone crosses into the fetal circulation. When your doctor considers either of these drugs crucial, their potential benefits must be carefully weighed against their risks.
Jul
5
Corticosteroids in Arthritis Treatment
July 5, 2009 | Leave a Comment
Corticosteroids
When cortisone was first introduced in the 1950s it was heralded as a wonder drug. Doctors became overnight heroes because they helped patients who had been crippled by rheumatoid arthritis get out of bed and begin functioning again. Even people with milder conditions like osteoarthritis, aller-
COMMON CORTICOSTEROIDS
• Cortisone
• Dexamethasone
• Hydrocortisone
• Methylprednisolone
• Prednisolone
• Prednisone
• Triamcinolone
• Cataracts
• Osteoporosis
• Diabetes
• Spontaneous fractures
• Bone deterioration
• Insomnia
• Irritability
• Glaucoma
• Fluid retention
• Weight gain
• Moon face
CORTICOSTEROIDS
• Infections
• High blood pressure
• Blood clots
• Potassium loss
• Stomach ulcers
• Muscle weakness
• Menstrual disturbances
• Impaired wound healing
• Fatigue
• Steroid “psychosis”
gies, asthma, and eczema were thrilled because corticosteroids relieved their symptoms amazingly well. But the very reason these medications were so successful was also their Achilles’ heel. As great as they are at easing inflammation, they profoundly affect cells throughout the body. Taking high doses for long periods of time is a little like dancing with the devil.
Once people woke up to the downside of steroids, the drugs lost their luster and fell into disfavor. Don’t get us wrong, though. These medications are incredibly valuable, especially for short-term use. People experiencing an arthritis flare-up, a bad ’sunburn, or a terrible case of poison ivy will benefit im- mensely from a pulsed dose of corticosteroids. When Joe went deaf in one ear, a course of prednisone restored his hearing. If used cautiously and with respect for their risks, these drugs can be extremely valuable. But using corticosteroids regularly to treat arthritis is a slippery slope.
Jul
3
Leukotriene Modifier Montelukast (Singulair)
We used to think Singulair was a very cool drug. It is an oral prescription medicine that blocks the effects of those inflammatory chemicals called leukotrienes. So, it only made sense to us that a drug like Singulair would relieve symptoms. This medication is widely prescribed to ease the breathing problems associated with asthma.
Research suggests, however, that Singulair is only modestly effective for alleviating itching, sneezing, congestion, and runny nose. It is roughly comparable to antihistamines such as loratadine (Claritin). One study reported that Singu-
***** Corticosteroid Nasal Sprays
Most allergy experts believe that these steroid sprays are the most effective treatments available and should be the first-line therapy. They are not likely to cause drowsiness or sedation and should be safe for people who must drive or operate machinery.
Side effects: Nasal irritation, stinging, burning, and bleeding. Other adverse reactions may include sore throat (and, rarely, yeast infections), headache, nausea, and cough. Rare adverse reactions may include perforation of the septum, nasal ulcers, reduced growth. rate in children, glaucoma, cataracts, and asthma symptoms.
Downside: These drugs are pricey and may alter the senses of taste and smell.
Cost: Approximately $85 to $95 for brand•name nasal sprays. Generic flunisolide is $35 to $40 per bottle.
lair, which costs more than $3 per pill, was no more effective than the oral decongestant pseudoephedrine (Sudafed) for relieving typical allergy symptoms. 56 Generic pseudoephedrine is far less expensive than Singulair. It is harder to purchase these days because pharmacists can only dispense it from behind the counter. You don’t need a prescription, but you will have to sign for it. Too many people used pseudoephedrine to make the illegal drug methamphetamine, so states and the federal government cracked down on easy access.
The research demonstrating that pseudoephedrine is quite effective in relieving allergy symptoms has forced us to reevaluate this old and inexpensive vasoconstrictor. It works by shrinking blood vessels in the nose. Perhaps that’s why so many drug companies now add this OTC ingredient to their antihistamines. Whenever you see a D appended to the name of an allergy medicine, you can pretty much assume that there is a decongestant on board, and frequently it is pseudoephedrine. It is found in Allegra-D, Claritin-D, Clarinex-D, Zyrtec-D, and other similar formulations.
O.I would like to point out a side effect of allergy medications that contain pseudoephedrine for nasal decongestion. Taking Claritin-D left me completely unable to fall asleep. I was literally up all night with a racing heartbeat.
I have had insomnia problems before, so I did not immediately associate this with the medication and continued to take it for 5 days. I was so sleep deprived that I couldn’t work.
I finally read the warning about nervousness, dizziness, or sleeplessness. I called my doctor, who said I should switch to Claritin (non-D). On this drug I sleep like a baby.
I found that some OTC allergy medicines I had taken for years also contain pseudoephedrine. I suspect this contributed to my earlier insomnia problems.
I urge anyone with insomnia to check all medications for pseudoephedrine. It does not affect everyone, but some of us just can’t handle even a small amount.
A. Millions of people struggle with insomnia and many don’t realize that the medicines they take may be contributing to their problem.
Decongestants aren’t the only culprits. Antihistamines, antidepressants, asthma medicines, blood pressure pills, and pain relievers are some of the drugs that can cause insomnia.
As popular as pseudoephedrine may be, there are some side effects to be alert for. Many people complain of insomnia, anxiety, agitation, headache, nausea, dizziness, and tremor. The most serious adverse reactions are elevated blood pressure and irregular heart rhythms. Men with prostate enlargement must avoid this decongestant because it can make urination much more difficult.
Jul
3
Allergy: Corticosteroid Nasal Sprays
July 3, 2009 | Leave a Comment
Corticosteroid Nasal Sprays
The big revolution in allergy treatment involves the use of steroid nasal sprays. Allergists have known for decades that cortisone-like drugs (prednisone, for example) can dampen the reactions of an overactive immune system and calm allergy symptoms amazingly well. The trouble is that relief comes at a stiff price. So many side effects are associated with oral corticosteroids that few physicians would ever consider prescribing such medications for nasal allergy symptoms except as a last resort. Even then, cautious doctors prescribe medications like prednisone for the shortest period of time necessary. Adverse reactions can include irritability, insomnia, anxiety, high blood pressure, potassium depletion, headache, nausea, and dizziness.
Not surprisingly, people wanted the benefits of steroids without the risks. That’s where nasal sprays come in. There are about a half- dozen different intranasal corticosteroids available by prescription. Most experts would say that these formulations are the most effective allergy treatment available. Although it may take a week for the benefits to reach peak effect, these sprays should relieve allergy symptoms such as itching, sneezing, and congestion quite well. They are pricey, however. A small bottle can run $85 to $95. At the time of this writing, generic flunisolide costs around $40. We cannot say whether one spray is better or safer than another.
The general consensus is that there are few, if any, systemic
GENERIC
BRAND NAME
Beclomethasone
Beconase AQ
Budesonide
Rhinocort Aqua
Flunisolide
Nasarel
Fluticasone
Flonase
Mometasone
Nasonex
Nasacort AQ
Triamcinolone
INTRANASAL
CORTICOSTEROIDS
side effects associated with topical steroids. In other words, the experts do not believe people absorb enough of the drugs into the system to cause much, if any, concern.55 One study did report growth suppression in children, but other research has not confirmed this complication. There have been rare reports of nasal perforation (creating a hole between the nostrils) and increased pressure within the eyes. More common are local reactions such as irritation and burning in the nose, sore throat, nasal dryness, nosebleed, and headache.
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