Acetaminophen

Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD

BRAND NAME: Tylenol and others

DRUG CLASS AND MECHANISM: Acetaminophen belongs to a class of drugs called analgesics (pain relievers) and antipyretics (fever reducers). The exact mechanism of action of acetaminophen is not known. Acetaminophen relieves pain by elevating the pain threshold, that is, by requiring a greater amount of pain to develop before a person feels it. It reduces fever through its action on the heat-regulating center of the brain. Specifically, it tells the center to lower the body's temperature when the temperature is elevated. The FDA approved acetaminophen in 1951.

PRESCRIPTION: No.

GENERIC AVAILABLE: Yes.

PREPARATIONS: Liquid suspension, chewable tablets, coated caplets, gelcaps, geltabs, and suppositories. Common dosages are 325, 500 and 650 mg.

STORAGE: Store tablets and solutions at room temperature 15°-30°C (59°-86°F). Suppositories should be refrigerated below 27°C (80°F).

PRESCRIBED FOR: Acetaminophen is used for the relief of fever as well as aches and pains associated with many conditions. Acetaminophen relieves pain in mild arthritis but has no effect on the underlying inflammation, redness, and swelling of the joint. If the pain is not due to inflammation, acetaminophen is as effective as aspirin. It is as effective as the non-steroidal antiinflammatory drug ibuprofen (Motrin) in relieving the pain of osteoarthritis of the knee. Unless directed by physician, acetaminophen should not be used for longer than 10 days.

DOSING: The oral dose for adults is 325 to 650 mg every 4 to 6 hours. The maximum daily dose is 4 grams. The oral dose for a child is based on the child's age, and the range is 40-650 mg every 4 hours.

When administered as a suppository, the adult dose is 650 mg every 4 to 6 hours. For children, the dose is 80-325 mg every 4 to 6 hours depending on age.

DRUG INTERACTIONS: Acetaminophen is metabolized (eliminated by conversion to other chemicals) by the liver. Therefore drugs that increase the action of liver enzymes that metabolize acetaminophen [for example, carbamazepine (Tegretol), isoniazid (INH, Nydrazid, Laniazid), rifampin (Rifamate, Rifadin, Rimactane)] reduce the levels of acetaminophen and may decrease the action of acetaminophen. Doses of acetaminophen greater than the recommended doses are toxic to the liver and may result in severe liver damage. The potential for acetaminophen to harm the liver is increased when it is combined with alcohol or drugs that also harm the liver.

Cholestyramine (Questran) reduces the effect of acetaminophen by decreasing its absorption into the body from the intestine. Therefore, acetaminophen should be administered 3 to 4 hours after cholestyramine or one hour before cholestyramine .

Acetaminophen doses greater than 2275 mg per day may increase the blood thinning effect of warfarin (Coumadin) by an unknown mechanism. Therefore, prolonged administration or large doses of acetaminophen should be avoided during warfarin therapy.

PREGNANCY: Acetaminophen is used in all stages of pregnancy and is the drug of choice for short-term treatment of fever and minor pain during pregnancy.

NURSING MOTHERS: Acetaminophen is excreted in breast milk in small quantities. However, acetaminophen use by the nursing mother appears to be safe.

SIDE EFFECTS: When used appropriately, side effects with acetaminophen are rare. The most serious side effect is liver damage due to large doses, chronic use or concomitant use with alcohol or other drugs that also damage the liver. Chronic alcohol use may also increase the risk of stomach bleeding.

Source emedicine.com

Tramadol

Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD

BRAND NAME: Ultram

DRUG CLASS AND MECHANISM: Tramadol is a man-made (synthetic) analgesic (pain reliever). Its exact mechanism of action is unknown but similar morphine. Like morphine, tramadol binds to receptors in the brain (opioid receptors) that are important for transmitting the sensation of pain from throughout the body to. Tramadol, like other narcotics used for the treatment of pain, may be abused. Tramadol is not a nonsteroidal antiinflammatory drug (NSAID) and does not have the increased risk of stomach ulceration and internal bleeding that can occur with NSAIDs.

PRESCRIPTION: Yes

GENERIC AVAILABLE: Yes

PREPARATIONS: Tablets (immediate release): 50 mg. Tablets (extended release): 100, 200, and 300 mg.

STORAGE: Store at room temperature, 15-30°C (59-86°F). Store in a sealed container.

PRESCRIBED FOR: Tramadol is used in the management of moderate to moderately severe pain. Extended release tablets are used for moderate to moderately severe chronic pain in adults who require continuous treatment for an extended period.

DOSING: The recommended dose of tramadol is 50-100 mg (immediate release tablets) every 4-6 hours as needed for pain. The maximum dose is 400 mg/day. To improve tolerance patients should be started at 25 mg/day, and doses may be increased by 25 mg every 3 days to reach 100 mg/day (25 mg 4 times daily). Thereafter, doses can be increased by 50 mg every 3 days to reach 200 mg day (50 mg 4 times daily). Tramadol may be taken with or without food.

Recommended dose for extended release tablets is 100 mg daily which may be increased by 100 mg every 5 days but not to exceed 300 mg /day. Extended release tablets should be swallowed whole and not crushed or chewed.

DRUG INTERACTIONS: Carbamazepine reduces the effect of tramadol by increasing its inactivation in the body. Quinidine (Quinaglute, Quinidex) reduces the inactivation of tramadol, thereby increasing the concentration of tramadol by 50%-60%. Combining tramadol with monoamine oxidase inhibitors (for example, Parnate) or selective serotonin inhibitors [(SSRIs, for example, fluoxetine (Prozac)] may result in severe side effects such as seizures or a condition called serotonin syndrome.

Tramadol may increase central nervous system and respiratory depression when combined with alcohol, anesthetics, narcotics, tranquilizers or sedative hypnotics.

PREGNANCY: The safety of tramadol during pregnancy has not been established.

NURSING MOTHERS: The safety of tramadol in nursing mothers has not been established.

SIDE EFFECTS: Tramadol is generally well tolerated, and side effects are usually transient. Commonly reported side effects include nausea, constipation, dizziness, headache, drowsiness, and vomiting. Less commonly reported side effects include itching, sweating, dry mouth, diarrhea, rash, visual disturbances, and vertigo. Some patients who received tramadol have reported seizures. Abrupt withdrawal of tramadol may result in anxiety, sweating, insomnia, rigors, pain, nausea, diarrhea, tremors, and hallucinations.

Source emedicine.com

Prednisone

Pharmacy Author: Omudhome Ogbru, Pharm.D.
Medical Editor: Jay Marks, M.D.

BRAND NAME: Deltasone, Orasone, Prednicen-M, Liquid Pred

DRUG CLASS AND MECHANISM: Prednisone is an oral, synthetic (man-made) corticosteroid used for suppressing the immune system and inflammation. It has effects similar to other corticosteroids such as triamcinolone (Kenacort), methylprednisolone (Medrol), prednisolone (Prelone) and dexamethasone (Decadron). These synthetic corticosteroids mimic the action of cortisol (hydrocortisone), the naturally-occurring corticosteroid produced in the body by the adrenal glands. Corticosteroids have many effects on the body, but they most often are used for their potent anti-inflammatory effects, particularly in those conditions in which the immune system plays an important role. Such conditions include arthritis, colitis, asthma, bronchitis, certain skin rashes, and allergic or inflammatory conditions of the nose and eyes. Prednisone is inactive in the body and, in order to be effective, first must be converted to prednisolone by enzymes in the liver. Therefore, prednisone may not work as effectively in people with liver disease whose ability to convert prednisone to prednisolone is impaired

PRESCRIPTION: yes

GENERIC AVAILABLE: yes

PREPARATIONS: Tablets of 2.5, 5, 10, 20, and 50 mg. Oral solution or syrup of 5mg/5ml

STORAGE: Store at room temperature 20-25°C (68-77°F), and keep away from moisture.

PRESCRIBED FOR: Prednisone is used in the management of inflammatory conditions or diseases in which the immune system plays an important role. Since prednisone is used in so many conditions, only the most common or established uses are mentioned here. Prednisone most often is used for treating several types of arthritis, ulcerative colitis, Crohn's disease, systemic lupus, allergic reactions, asthma and severe psoriasis. It also is used for treating leukemias, lymphomas, idiopathic thrombocytopenic purpura and autoimmune hemolytic anemia. Corticosteroids, including prednisone, are commonly used to suppress the immune system and prevent the body from rejecting transplanted organs. Prednisone is used as replacement therapy in patients whose adrenal glands are unable to produce sufficient amounts of cortisol.

DOSING: The initial dose of prednisone varies depending on the condition being treated and the age of the patient. The starting dose may be from 5 to 60 mg per day and often is adjusted based on the response of the condition being treated. Corticosteroids typically do not produce immediate effects and must be used for several days before maximal effects are seen. It may take much longer before conditions respond to treatment. Prolonged therapy with prednisone causes the adrenal glands to atrophy and stop producing cortisol. When prednisone is discontinued after a period of prolonged therapy, the dose of prednisone must be tapered (lowered gradually) to allow the adrenal glands time to recover. (See side effects.) It is recommended that prednisone be taken with food.

DRUG INTERACTIONS: Prednisone may interact with estrogens and phenytoin (Dilantin). Estrogens may reduce the action of enzymes in the liver that break down (eliminate) the active form of prednisone, prednisolone. As a result, the levels of prednisolone in the body may increase and lead to more frequent side effects. Phenytoin increases the activity of enzymes in the liver that break down (eliminate) prednisone and thereby may reduce the effectiveness of prednisone. Thus, if phenytoin is being taken, an increased dose of prednisone may be required.

PREGNANCY: Corticosteroids cross the placenta into the fetus. Compared to other corticosteroids, however, prednisone is less likely to cross the placenta. Chronic use of corticosteroids during the first trimester of pregnancy may cause cleft palate.

NURSING MOTHERS: Corticosteroids are secreted in breast milk and can cause side effects in the nursing infant. Prednisone is less likely than other corticosteroids to be secreted in breast milk, but it may still pose a risk to the infant.

SIDE EFFECTS: Side effects of prednisone and other corticosteroids range from mild annoyances to serious, irreversible damage, and they occur more frequently with higher doses and more prolonged treatment. Side effects include retention of sodium (salt) and fluid, weight gain, high blood pressure, loss of potassium, headache and muscle weakness. Prednisone also causes puffiness of the face (moon face), growth of facial hair, thinning and easy bruising of the skin, impaired wound healing, glaucoma, cataracts, ulcers in the stomach and duodenum, worsening of diabetes, irregular menses, rounding of the upper back ("buffalo hump"), obesity, retardation of growth in children, convulsions, and psychiatric disturbances. The psychiatric disturbances include depression, euphoria, insomnia, mood swings, personality changes, and even psychotic behavior.

Prednisone suppresses the immune system and, therefore, increases the frequency or severity of infections and decreases the effectiveness of vaccines and antibiotics. Prednisone may cause osteoporosis that results in fractures of bones. Patients taking long-term prednisone often receive supplements of calcium and vitamin D to counteract the effects on bones. Calcium and vitamin D probably are not enough, however, and treatment with bisphosphonates such as alendronate (Fosamax) and risedronate (Actonel) may be necessary. Calcitonin (Miacalcin) also is effective. The development of osteoporosis and the need for treatment can be monitored using bone density scans.

Prolonged use of prednisone and other corticosteroids causes the adrenal glands to atrophy (shrink) and stop producing the body's natural corticosteroid, cortisol. If prednisone is abruptly withdrawn after prolonged use, the adrenal glands are unable to produce enough cortisol to compensate for the withdrawal, and symptoms of corticosteroid insufficiency (adrenal crisis) may occur. These symptoms include nausea, vomiting and shock. Therefore, prednisone should be discontinued gradually so that the adrenal glands have time to recover and resume production of cortisol. Until the glands fully recover, it may be necessary to treat patients who have recently discontinued corticosteroids with a short course of corticosteroids during times of stress (infection, surgery, etc.), times when corticosteroids are particularly important to the body.

A serious complication of long-term use of corticosteroids is aseptic necrosis of the hip joints. Aseptic necrosis is a condition in which there is death and degeneration of the hip bone. It is a painful condition that ultimately can lead to the need for surgical replacement of the hip. Aseptic necrosis also has been reported in the knee joints. The estimated incidence of aseptic necrosis among long-term users of corticosteroids is 3-4%. Patients taking corticosteroids who develop pain in the hips or knees should report the pain to their doctors promptly.

Source emedicine.com

Amoxicillin

Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD

BRAND NAME: Amoxil, Dispermox, Trimox

DRUG CLASS AND MECHANISM: Amoxicillin belongs to a class of antibiotics called penicillins. Other members of this class include ampicillin (Unasyn), piperacillin (Pipracil), ticarcillin (Ticar) and several others. These antibiotics all have a similar mechanism of action. They do not kill bacteria, but they stop bacteria from multiplying by preventing bacteria from forming the walls that surround them. The walls are necessary to protect bacteria from their environment and to keep the contents of the bacterial cell together. Bacteria cannot survive without a cell wall. Amoxicillin is effective against many different bacteria including H. influenzae, N. gonorrhoea, E. coli, Pneumococci, Streptococci, and certain strains of Staphylococci.

PRESCRIPTION: Yes.

GENERIC AVAILABLE: Yes.

PREPARATIONS: Capsules: 250 and 500 mg. Tablets: 500 and 875 mg. Chewable tablets: 125, 200, 250, and 400 mg. Powder for suspension: 50 mg/ml ; 125, 200, 250, and 400 mg/5 ml. Tablets for suspension: 200 and 400 mg

STORAGE: Store Amoxil capsules as well as 125 and 250 mg dry powder at or below 20°C (68°F); tablets, chewable tablets, as well as 200 and 400 mg dry powder should be stored at or below 25°C(77°F). Store Trimox capsules and unreconstituted powder at or below 20°C (68°F) and chewable tablets at room temperature 15°-30°C (59°-86°F). Powder that has been mixed with water should be discarded after 14 days. Refrigeration is preferred but not required for powder mixed with water.

PRESCRIBED FOR: Amoxicillin is used to treat infections due to organisms that are susceptible to the effects of amoxicillin. Common infections that amoxicillin is used for include infections of the middle ear, tonsils, throat, larynx (laryngitis), bronchi (bronchitis), lungs (pneumonia), urinary tract, and skin. It also is used to treat gonorrhea.

DOSING: For most infections in adults the dosing regimens for amoxicillin are 250 mg every 8 hours, 500 mg every 8 hours, 500 mg every 12 hours or 875 mg every 12 hours, depending on the type and severity of infection.

For the treatment of adults with gonorrhea, the dose is 3 g given as one dose.

For most infections, children older than 3 months but less than 40 kg are treated with 25 mg/kg/day in divided doses every 12 hours, 20 mg/kg/day in divided doses every 8 hours, 40 mg/kg/day in divided doses every 8 hours or 45 mg/kg/day in divided doses every 12 hours depending on type and severity of the infection.

Amoxicillin can be taken with or without food.

DRUG INTERACTIONS: Amoxicillin is rarely associated with important drug interactions.

PREGNANCY: Penicillins are generally considered safe for use by pregnant women who are not allergic to penicillin.

NURSING MOTHERS: Small amounts of amoxicillin may be excreted in breast milk and may cause diarrhea or allergic responses in nursing infants. Amoxicillin is generally considered safe to use while breastfeeding. Amoxicillin is used to treat infections in the newborn.

SIDE EFFECTS: Side effects due to amoxicillin include diarrhea, dizziness, heartburn, insomnia, nausea, itching, vomiting, confusion, abdominal pain, easy bruising, bleeding, rash, and allergic reactions. Individuals who are allergic to antibiotics in the class of cephalosporins may also be sensitive to amoxicillin.

Source emedicine.com

Ibuprofen

Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD

BRAND NAME: Advil, Children's Advil/Motrin, Medipren, Motrin, Nuprin, PediaCare Fever etc.

DRUG CLASS AND MECHANISM: Ibuprofen belongs to a class of drugs called non-steroidal anti-inflammatory drugs (NSAIDs). Other members of this class include aspirin, naproxen (Aleve), indomethacin (Indocin), nabumetone (Relafen) and several others. These drugs are used for the management of mild to moderate pain, fever, and inflammation. Pain, fever, and inflammation are promoted by the release in the body of chemicals called prostaglandins. Ibuprofen blocks the enzyme that makes prostaglandins (cyclooxygenase), resulting in lower levels of prostaglandins. As a consequence, inflammation, pain and fever are reduced. The FDA approved ibuprofen in 1974.

PRESCRIPTION: Yes

GENERIC AVAILABLE: Yes

PREPARATIONS: Tablets of 200, 400, 600, and 800 mg; Chewable tablets of 50 and 100 mg; Capsules of 200 mg; Suspension of 100 mg/2.5 ml and 100 mg/5 ml; Oral drops of 40 mg/ml.

STORAGE: Ibuprofen should be stored at room temperature, between 15-30°C (59-86°F).

PRESCRIBED FOR: Ibuprofen is used for the treatment of mild to moderate pain, inflammation and fever caused by many and diverse diseases.

DOSING: For minor aches, mild to moderate pain, menstrual cramps, and fever, the usual adult dose is 200 or 400 mg every 4 to 6 hours.

Arthritis is treated with 300 to 800 mg 3 or 4 times daily.

When under the care of a physician, the maximum dose of ibuprofen is 3.2 g daily. Otherwise, the maximum dose is 1.2 g daily. Individuals should not use ibuprofen for more than 10 days for the treatment of pain or more than 3 days for the treatment of a fever unless directed by a physician.

Children 6 months to 12 years of age usually are given 5-10 mg/kg of ibuprofen every 6-8 hours for the treatment of fever and pain. The maximum dose is 40 mg/kg daily.

Juvenile arthritis is treated with 20 to 40 mg/kg/day in 3-4 divided doses.

Ibuprofen should be taken with meals to prevent stomach upset.

DRUG INTERACTIONS: Ibuprofen is associated with several suspected or probable interactions that can affect the action of other drugs. Ibuprofen may increase the blood levels of lithium (Eskalith) by reducing the excretion of lithium by the kidneys. Increased levels of lithium may lead to lithium toxicity. Ibuprofen may reduce the blood pressure-lowering effects of drugs that are given to reduce blood pressure. This may occur because prostaglandins play a role in the regulation of blood pressure. When ibuprofen is used in combination with aminoglycosides [for example, gentamicin (Garamycin)] the blood levels of the aminoglycoside may increase, presumably because the elimination of aminoglycosides from the body is reduced. This may lead to aminoglycoside-related side effects. Individuals taking oral blood thinners or anticoagulants [for example, warfarin (Coumadin)] should avoid ibuprofen because ibuprofen also thins the blood, and excessive blood thinning may lead to bleeding.

PREGNANCY: There are no adequate studies of ibuprofen in pregnant women. Therefore, ibuprofen is not recommended during pregnancy. Ibuprofen should be avoided in late pregnancy due to the risk of premature closure of the ductus arteriosus in the fetal heart..

NURSING MOTHERS: Ibuprofen is not excreted in breast milk. Use of ibuprofen while breastfeeding, poses little risk to the infant.

SIDE EFFECTS: The most common side effects from ibuprofen are rash, ringing in the ears, headaches, dizziness, drowsiness, abdominal pain, nausea, diarrhea, constipation and heartburn. NSAIDs reduce the ability of blood to clot and therefore increase bleeding after an injury. Ibuprofen may cause ulceration of the stomach or intestine, and the ulcers may bleed. Sometimes, ulceration can occur without abdominal pain, and black, tarry stools, weakness, and dizziness upon standing (orthostatic hypotension) due to bleeding may be the only signs of an ulcer. NSAIDs reduce the flow of blood to the kidneys and impair function of the kidneys. The impairment is most likely to occur in patients who already have impaired function of the kidney or congestive heart failure, and use of NSAIDs in these patients should be cautious. People who are allergic to other NSAIDs, including aspirin, should not use ibuprofen. Individuals with asthma are more likely to experience allergic reactions to ibuprofen and other NSAIDs. Fluid retention (edema), blood clots, heart attacks, hypertension and heart failure have also been associated with the use of NSAIDs.

Source emedicine.com

Angiotensin Converting Enzyme (ACE) Inhibitors

Pharmacy Author: Omudhome Ogbru, Pharm.D.
Medical Editor: Jay W. Marks, M.D.

What are ACE inhibitors, and how do they work?

Angiotensin II is a very potent chemical that causes the muscles surrounding blood vessels to contract and thereby narrows the blood vessels. The narrowing of the vessels increases the pressure within the vessels and can cause high blood pressure (hypertension). Angiotensin II is formed from angiotensin I in the blood by the enzyme, angiotensin converting enzyme (ACE). ACE inhibitors are medications that slow (inhibit) the activity of the enzyme, which decreases the production of angiotensin II. As a result, the blood vessels enlarge or dilate, and the blood pressure is reduced. This lower blood pressure makes it easier for the heart to pump blood and can improve the function of a failing heart. In addition, the progression of kidney disease due to high blood pressure or diabetes is slowed.

For what conditions are ACE inhibitors used?

ACE inhibitors are used for controlling blood pressure, treating heart failure and preventing kidney damage in people with hypertension or diabetes. They also benefit patients who have had heart attacks. In studies, individuals with hypertension, heart failure, or prior heart attacks who were treated with an ACE inhibitor lived longer than patients who did not take an ACE inhibitor. Because they prevent early death resulting from hypertension, heart failure or heart attacks, ACE inhibitors are one of the most important group of drugs. Some individuals with hypertension do not respond sufficiently to ACE inhibitors alone. In these cases, other drugs are used in combination with ACE inhibitors.

Are there any differences among the different types of ACE inhibitors?

ACE inhibitors are very similar. However, they differ in how they are eliminated from the body and their doses. Some ACE inhibitors need to be converted into an active form in the body before they work. In addition, some ACE inhibitors may work more on ACE that is found in tissues than on ACE that is present in the blood. The importance of this difference or whether one ACE inhibitor is better than another, has not been determined.

What are the side effects of ACE inhibitors?

ACE inhibitors are relatively well-tolerated by most individuals. Nevertheless, they are not free of side effects, and some patients should not use ACE inhibitors. ACE inhibitors usually are not prescribed for pregnant patients because they may cause birth defects. Individuals with severe kidney problems and people who have had a severe reaction to ACE inhibitors probably should avoid them. The most common side effects are cough, elevated blood potassium levels, low blood pressure, dizziness, headache, drowsiness, weakness, abnormal taste (metallic or salty taste), and rash. It may take up to a month for coughing to subside, and if one ACE inhibitor causes cough it is likely that the others will too. The most serious, but rare, side effects of ACE inhibitors are kidney failure, allergic reactions, a decrease in white blood cells, and swelling of tissues (angioedema).

With which drugs do ACE inhibitors interact?

ACE inhibitors have few interactions with other drugs. Since ACE inhibitors may increase blood levels of potassium, the use of potassium supplements, salt substitutes (which often contain potassium), or other drugs that increase the body's potassium may result in excessive blood potassium levels. ACE inhibitors also may increase the blood concentration of lithium (Eskalith) and lead to an increase in side effects from lithium. There have been reports that aspirin and other non-steroidal anti-inflammatory drugs (NSAIDS) such as ibuprofen, indomethacin, and naproxen may reduce the effects of ACE inhibitors; however, there is no conclusive evidence that this interaction, if it exists, is important.

What ACE inhibitors are available?

The following is a list of the ACE inhibitors that are available in the United States:

captopril (Capoten), benazepril (Lotensin), enalapril (Vasotec), lisinopril (Prinivil, Zestril) fosinopril (Monopril), ramipril (Altace), perindopril (Aceon), quinapril (Accupril), moexipril (Univasc), and trandolapril (Mavik).

Source emedicine.com