A

A



abacavir sulfate


(a-ba-ka’-vir sul’-fate)


image Brand Name(s): Ziagen


Combinations

Rx: with lamivudine (Epzicom); with zidovudine and lamivudine (Trizivir)

Chemical Class: Nucleoside analog

image Clinical Pharmacology:


Mechanism of Action: An antiretroviral that inhibits the activity of HIV-1 reverse transcriptase by competing with the natural substrate deoxyguanosine-5′-triphosphate (dGTP) and by its incorporation into viral DNA. Therapeutic Effect: Inhibits viral DNA growth.

Pharmacokinetics: Rapidly and extensively absorbed after PO administration. Protein binding: 50%. Widely distributed, including to CSF and erythrocytes. Metabolized in the liver to inactive metabolites. Primarily excreted in urine. Unknown if removed by hemodialysis. Half-life: 1.5 hr.

image Available Forms:


• Tablets: 300 mg.

• Oral Solution: 20 mg/ml.

image Indications and Dosages:


HIV infection (in combination with other ID-antiretrovirals): PO 300 mg twice a day or 600 mg once daily.

Dosage in hepatic impairment: Mild impairment: 200 mg twice a day. Moderate to severe impairment: Not recommended.

image Contraindications: Moderate or severe hepatic impairment



image Side Effects



Frequent

Nausea (47%), nausea with vomiting (16%), diarrhea (12%), decreased appetite (11%)

Occasional

Insomnia (7%)


image Serious Reactions



• A hypersensitivity reaction may be life-threatening. Signs and symptoms include fever, rash, fatigue, intractable nausea and vomiting, severe diarrhea, abdominal pain, cough, pharyngitis, and dyspnea.

• Life-threatening hypotension may occur.

• Lactic acidosis and severe hepatomegaly may occur.


Special Considerations



• Always check updated treatment guidelines before initiating or changing antiretroviral therapy. (http://AIDSinfo.nih.gov)


image Patient/Family Education



• May administer without regard for food

• If you miss a dose: take the missed dose as soon as you remember, then go back to your normal dosing schedule; skip the missed dose if it is time for your next dose; do not take 2 doses at the same time

• Do not take any other medication, including OTC drugs, without consulting the physician

• Abacavir is not a cure for HIV infection, nor does it reduce the risk of transmitting HIV to others


image Monitoring Parameters



• CBC, metabolic panel, CD4 lymphocyte count, HIV RNA level

• Pattern of daily bowel activity and stool consistency

• Weight

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls


image U.S. Regulatory Considerations



image FDA Black Box

Hypersensitivity Reactions: severe and fatal reactions associated with therapy. This drug should never be restarted after suspected hypersensitivity reaction as more severe symptoms can occur within hours and may include life-threatening hypotension and death. Severe or fatal reaction may occur within hrs after reintroduction of drug in patients with unrecognized symptoms of hypersensitivity.

image OBRA regulated in U.S. Long Term Care


abciximab


(ab-siks’-ih-mab)


image Brand Name(s): ReoPro


Chemical Class: Glycoprotein (GP) IIb/IIIa inhibitor

image Clinical Pharmacology:


Mechanism of Action: A glycoprotein IIb/IIIa receptor inhibitor that rapidly inhibits platelet aggregation by preventing the binding of fibrinogen to GP IIb/IIIa receptor sites on platelets. Therapeutic Effect: Prevents closure of treated coronary arteries. Prevents acute cardiac ischemic complications.

Pharmacokinetics: Rapidly cleared from plasma. Initial-phase half-life is less than 10 min; second-phase half-life is 30 min. Platelet function generally returns within 48 hr.

image Available Forms:


• Injection: 2 mg/ml (5-ml vial).

image Indications and Dosages:


Percutaneous coronary intervention (PCI): IV Bolus 0.25 mg/kg 10-60 min before angioplasty or atherectomy, then 12-hr IV infusion of 0.125 mcg/kg/min. Maximum: 10 mcg/min.

PCI (unstable angina): IV Bolus 0.25 mg/kg, followed by 18- to 24-hr infusion of 10 mcg/min, ending 1 hr after procedure.

image Contraindications: Active internal bleeding, arteriovenous malformation or aneurysm, cerebrovascular accident (CVA) with residual neurologic defect, history of CVA (within the past 2 yr) or oral anticoagulant use within the past 7 days unless PT is less than 1.2 × control, history of vasculitis, hypersensitivity to murine proteins, intracranial neoplasm, prior IV dextran use before or during percutaneous transluminal coronary angioplasty (PTCA), recent surgery or trauma (within the past 6 wk), recent (within the past 6 wk or less) GI or GU bleeding, thrombocytopenia (less than 100,000 cells/μl), and severe uncontrolled hypertension



image Side Effects



Frequent

Nausea (16%), hypotension (12%)

Occasional (9%)

Vomiting

Rare (3%)

Bradycardia, confusion, dizziness, pain, peripheral edema, urinary tract infection


image Serious Reactions



• Major bleeding complications may occur. If complications occur, stop the infusion immediately.

• Hypersensitivity reaction may occur.

• Atrial fibrillation or flutter, pulmonary edema, and complete AV block occur occasionally.


Special Considerations



• Fab fragment of the chimeric human-murine monoclonal antibody 7E3

• Intended to be used with aspirin and heparin

• Discontinue if bleeding occurs that is not controlled by compression

• Discontinue if PTCA fails

• Eptifibatide, tirofiban, and abciximab can all decrease the incidence of cardiac events associated with acute coronary syndromes; direct comparisons are needed to establish which, if any, is superior; for angioplasty, until more data become available, abciximab appears to be the drug of choice


image Patient/Family Education



• Use an electric razor and soft toothbrush to prevent bleeding

• Report signs of bleeding, including black or red stool, coffee-ground emesis, red or dark urine, or red-speckled mucus from cough


image Monitoring Parameters



• Baseline platelet count, prothrombin time, aPTT; during INF closely monitor platelet count and aPTT (heparin therapy)

• Stop abciximab and heparin infusion if serious bleeding uncontrolled by pressure occurs

• Assess skin for ecchymosis and petechiae; also, assess for GI, GU, and retroperitoneal bleeding and for bleeding at all puncture sites

• Assess for signs and symptoms of hemorrhage, including a decrease in blood pressure, increase in pulse rate, abdominal or back pain, and severe headache

• Assess urine for hematuria

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls


image U.S. Regulatory Considerations



image FDA Black Box

Hypersensitivity reaction to this drug is a multi-organ clinical syndrome usually characterized by a sign or symptom in 2 or more of the following groups: 1) fever, 2) rash, 3) gastrointestinal (including nausea, vomiting, diarrhea, or abdominal pain), 4) constitutional (e.g., generalized malaise, fatigue, or achiness), and 5) respiratory (e.g., dyspnea, cough, or pharyngitis).

image OBRA regulated in U.S. Long Term Care


acamprosate calcium


(ah-camp’-ro-sate kal’-see-um)


image Brand Name(s): Campral


Chemical Class: Amino acid derivative

image Clinical Pharmacology:


Mechanism of Action: An alcohol abuse deterrent that appears to interact with glutamate and gamma-aminobutyric acid neurotransmitter systems centrally, restoring their balance. Therapeutic Effect: Reduces alcohol dependence.

Pharmacokinetics: Slowly absorbed from the GI tract. Steady-state plasma concentrations are reached within 5 days. Does not undergo metabolism. Excreted in urine. Half-life: 20-33 hr.

image Available Forms:


• Tablets: 333 mg.

image Indications and Dosages:


Maintenance of alcohol abstinence in alcohol-dependent patients who are abstinent at initiation of treatment: PO Two tablets 3 times a day.

Dosage in renal impairment: For patients with creatinine clearance of 30-49 ml/min, dosage is decreased to 1 tablet 3 times a day.

image Contraindications: Severe renal impairment (creatinine clearance of 30 ml/min or less)



image Side Effects



Frequent (17%)

Diarrhea

Occasional (6%-4%)

Insomnia, asthenia, fatigue, anxiety, flatulence, nausea, depression, pruritus

Rare (3%-1%)

Dizziness, anorexia, paresthesia, diaphoresis, dry mouth


image Serious Reactions



• Acute renal failure has been reported.


Special Considerations



• Does not cause disulfiram-like reaction with ingestion of alcohol

• Higher doses appear to be more effective for maintaining abstinence

• The optimal time to initiate therapy has not been identified


image Patient/Family Education



• Use caution operating hazardous machinery, including automobiles, until there is reasonable certainty that acamprosate will not affect ability to engage in such activities

• Continue use even in the event of a relapse and discuss any renewed drinking with prescriber

• To be used as part of a treatment program that includes psychosocial support


image Monitoring Parameters



• Maintenance of alcohol abstinence

• Pattern of daily bowel activity and stool consistency

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls


image U.S. Regulatory Considerations



image FDA Black Box

image OBRA regulated in U.S. Long Term Care


acarbose


(ay’-car-bose)


image Brand Name(s): Precose


Chemical Class: α-Amylase inhibitor; α-glucosidase inhibitor

image Clinical Pharmacology:


Mechanism of Action: An alpha-glucosidase inhibitor that delays glucose absorption and digestion of carbohydrates, resulting in a smaller rise in blood glucose concentration after meals. Therapeutic Effect: Lowers postprandial hyperglycemia.

Pharmacokinetics: Low absorption within the GI tract. Extensive metabolism in the intestinal wall. Degraded in the intestine by bacterial and digestive enzymes. Excreted in feces and urine. Half-life: 2 hr.

image Available Forms:


• Tablets: 25 mg, 50 mg, 100 mg.

image Indications and Dosages:


Diabetes mellitus: PO Initially, 25 mg 3 times a day with first bite of each main meal. May increase at 4- to 8-wk intervals. Maximum: For patients weighing more than 60 kg, 100 mg 3 times a day; for patients weighing 60 kg or less, 50 mg 3 times a day.

image Contraindications: Chronic intestinal diseases associated with marked disorders of digestion or absorption, cirrhosis, colonic ulceration, conditions that may deteriorate as a result of increased gas formation in the intestine, diabetic ketoacidosis, hypersensitivity to acarbose, inflammatory bowel disease, partial intestinal obstruction or predisposition to intestinal obstruction, significant renal dysfunction (serum creatinine level greater than 2 mg/dl)




image Side Effects


Side effects diminish in frequency and intensity over time.


Frequent


Transient GI disturbances: flatulence (77%), diarrhea (33%), abdominal pain (21%)



image Serious Reactions



• None known.


Special Considerations



• Does not cause hypoglycemia

• Reduces HbA1c 0.5%-1%

• Blood glucose; HbA1c 3-6 mo

• Consider ALT/AST during first yr


image Patient/Family Education



• Take glucose rather than complex carbohydrates to abort hypoglycemic episodes

• Decrease adverse GI effects by reducing dietary starch content

• Do not skip or delay meals

• Avoid alcohol

• Consult the physician when glucose demands are altered (such as with fever, heavy physical activity, infection, stress, trauma)

• Exercise, good personal hygiene (including foot care), not smoking, and weight control are essential parts of therapy


image Monitoring Parameters



• Food intake and blood glucose, glycosylated hemoglobin, and AST levels

• Assess for signs and symptoms of hypoglycemia (anxiety, cool wet skin, diplopia, dizziness, headache, hunger, numbness in mouth, tachycardia, tremors) or hyperglycemia (deep rapid breathing, dim vision, fatigue, nausea, polydipsia, polyphagia, polyuria, vomiting)

• Be alert to conditions that alter glucose requirements, including fever, increased activity or stress, or a surgical procedure

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls

Other: None

image Use with caution in older patients with: Impaired renal function



image U.S. Regulatory Considerations



image FDA Black Box

image OBRA regulated in U.S. Long Term Care

image Other Uses in Geriatric Patient: None


image Side Effects:


Of particular importance in the geriatric patient: Flatulence, abdominal discomfort, diarrhea

image Geriatric Considerations – Summary: GI effects may be even more prevalent in older adults. Not associated with hypoglycemia when used as monotherapy. If hypoglycemia occurs in a patient taking acarbose, use oral glucose for treatment as acorbose may prevent the absorption of other complex carbohydrates. Avoid in older adults with SCr >2 mg/dl.



References



1 Haas L. Management of diabetes mellitus medications in the nursing home. Drugs & Aging. 2005;22:209-218.


2 Rosenstock J. Management of type 2 diabetes mellitus in the elderly: special considerations. Drugs & Aging. 2001;18:31-44.



acebutolol hydrochloride


(a-se-byoo’-toe-lole hye-droe-klor’-ide)


image Brand Name(s): Sectral


Chemical Class: β1-Adrenergic blocker, cardioselective

image Clinical Pharmacology:


Mechanism of Action: A beta1-adrenergic blocker that competitively blocks beta1-adrenergic receptors in cardiac tissue. Reduces the rate of spontaneous firing of the sinus pacemaker and delays AV conduction. Therapeutic Effect: Slows heart rate, decreases cardiac output, decreases BP, and exhibits antiarrhythmic activity.

Pharmacokinetics:



image

Well absorbed from the GI tract. Protein binding: 26%. Undergoes extensive first-pass liver metabolism to active metabolite. Eliminated via bile, secreted into GI tract via intestine, and excreted in urine. Removed by hemodialysis. Half-life: 3-4 hr; metabolite, 8-13 hr.


image Available Forms:


• Capsules: 200 mg, 400 mg.

image Indications and Dosages:


Mild to moderate hypertension: PO Initially, 400 mg/day in 12 divided doses. Range: Up to 1200 mg/day in 2 divided doses. Maintenance: 400-800 mg/day.

Ventricular arrhythmias: PO Initially, 200-400 mg/day. Maximum: 800 mg/day.

Dosage in renal impairment: Dosage is modified based on creatinine clearance.













Creatinine Clearance % of Usual Dosage
less than 50 ml/min 50
less than 25 ml/min 25

image Unlabeled Uses: Treatment of anxiety, chronic angina pectoris, hypertrophic cardiomyopathy, MI, pheochromocytoma, syndrome of mitral valve prolapse, thyrotoxicosis, tremors


image Contraindications: Cardiogenic shock, heart block greater than first degree, overt heart failure, severe bradycardia



image Side Effects



Frequent

Hypotension manifested as dizziness, nausea, diaphoresis, headache, cold extremities, fatigue, constipation, or diarrhea

Occasional

Insomnia, urinary frequency, impotence or decreased libido

Rare

Rash, arthralgia, myalgia, confusion, altered taste


image Serious Reactions



• Overdose may produce profound bradycardia and hypotension.

• Abrupt withdrawal may result in diaphoresis, palpitations, headache, and tremors.

• Acebutolol administration may precipitate CHF or MI in patients with heart disease; thyroid storm in those with thyrotoxicosis; or peripheral ischemia in those with existing peripheral vascular disease.

• Hypoglycemia may occur in patients with previously controlled diabetes.

• Signs of thrombocytopenia, such as unusual bleeding or bruising, occur rarely.


Special Considerations



• Fewer CNS and bronchospastic effects than other beta-blockers


image Monitoring Parameters



• Heart rate, blood pressure

• ECG for arrhythmias

• Stool frequency and consistency, urine output

• Signs and symptoms of CHF


image Patient/Family Education



• Do not discontinue abruptly; may require taper; rapid withdrawal may produce rebound hypertension or angina

• Report excessive fatigue, headache, prolonged dizziness, shortness of breath, or weight gain

• Do not use nasal decongestants or OTC cold preparations (stimulants) without physician approval

• Restrict salt and alcohol intake

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls


image U.S. Regulatory Considerations



image FDA Black Box

In patients using orally administered beta-blockers, abrupt withdrawal may precipitate angina or lead to myocardial infarction or ventricular arrhythmias.

image OBRA regulated in U.S. Long Term Care


acetaminophen


(ah-seet’-ah-min-oh-fen)


image Brand Name(s):


OTC: Acephen, Apacet, Arthritis Pain Formula, Aspirin-Free Pain Relief, Feverall, Genapap, Liquiprin, Neopap, Panadol, Tapanol, Tempra, Tylenol

Combinations

Rx: with butalbital (Phrenilin); with butalbital and caffeine (Fioricet, Esgic, Isocet); with butalbital, caffeine, and codeine (Amaphen, Fioricet w/codeine); with codeine (Tylenol, Phenaphen No. 2,3,4); with dichloralphenazone and isometheptene (Midrin, Midchlor); with hydrocodone (Vicodin, Lorcet, Lortab); with oxycodone (Percocet, Roxicet, Tylox); with pentazocine (Talacen); with propoxyphene (Wygesic, Darvocet-N)

OTC: with pamabrom + pyrilamine (Midol PMS, Pamprin); with antihistamine and decongestant (Actifed Plus, Drixoral Cold & Flu, Benadryl Sinus, Sine-Off, Sinarest); with decongestant, antihistamine, dextromethorphan (Nyquil)

Chemical Class: Para-aminophenol derivative

image Clinical Pharmacology:


Mechanism of Action: A central analgesic whose exact mechanism is unknown, but appears to inhibit prostaglandin synthesis in the CNS and, to a lesser extent, block pain impulses through peripheral action. Acetaminophen acts centrally on hypothalamic heat-regulating center, producing peripheral vasodilation (heat loss, skin erythema, sweating). Therapeutic Effect: Results in antipyresis. Produces analgesic effect. Results in antipyresis.

Pharmacokinetics:



image

Rapidly, completely absorbed from GI tract; rectal absorption variable. Protein binding: 20%-50%. Widely distributed to most body tissues. Metabolized in liver; excreted in urine. Removed by hemodialysis. Half-life: 1-4 hr (half-life is increased in those with liver disease, elderly).


image Available Forms:


• Caplet (Genapap, Tylenol): 500 mg.

• Caplet, extended release (Mapap, Tylenol Arthritis Pain): 650 mg.

• Capsule (Mapap): 500 mg.

• Elixir: 160 mg/5 ml.

• Liquid, oral (Tylenol Extra Strength): 500 mg/15 ml.

• Suppository, rectal: 80 mg (Acephen, Feverall), 120 mg (Feverall), 325 mg (Feverall), 650 mg (Feverall).

• Tablet (Genapap, Mapap, Tylenol): 325 mg, 500 mg.

• Tablet, chewable (Genapap, Mapap, Tylenol): 80 mg.

image Indications and Dosages:


Analgesia and antipyresis: PO 325-650 mg q4-6h or 1g 3-4 times/day. Maximum: 4 g/day. Rectal 650 mg q4-6h. Maximum: 6 doses/24 hr.

Dosage in renal impairment:













Creatinine Clearance Frequency
10-50 ml/min q6h
Less than 10 ml/min q8h

image Contraindications: Active alcoholism, liver disease, or viral hepatitis, all of which increase the risk of hepatotoxicity




image Side Effects



Rare

Hypersensitivity reaction


image Serious Reactions



• Acetaminophen toxicity is the primary serious reaction.

• Early signs and symptoms of acetaminophen toxicity include anorexia, nausea, diaphoresis, and generalized weakness within the first 12-24 hr.

• Later signs of acetaminophen toxicity include vomiting, right upper quadrant tenderness, and elevated liver function tests within 48-72 hr after ingestion.

• The antidote to acetaminophen toxicity is acetylcysteine.


image Patient/Family Education



• Many OTC drugs contain acetaminophen; additive dosage may exceed 4 g/day maximum and increase risk of hepatotoxicity

• Consult with physician before using acetaminophen more than 10 days or for a fever lasting more than 3 days

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls

image Other: Elevated liver function studies

image Use with caution in older patients with: Hepatic impairment, daily alcohol use > 3 drinks per day



image U.S. Regulatory Considerations



image FDA Black Box

image OBRA regulated in U.S. Long Term Care

image Other Uses in Geriatric Patient: None


image Side Effects:


Of particular importance in the geriatric patient: None


image Geriatric Considerations – Summary



Preferred analgesic for mild to moderate pain in older adults due to safety profile. More effective in chronic pain when used on a scheduled basis. The extended-release product allows for q8h dosing, which may enhance compliance in patients taking acetaminophen for chronic pain.


Reference



1 Acetaminophen safety. Med Lett Drugs Ther. 2002;44:91-93.



acetaminophen; dichloralphenazone; isometheptene mucate


(ah-seet’-ah-min-oh-fen; dye-klor-al-fen’-a-zone; i-so-meh-thep’-tene)


image Brand Name(s): I.D.A, Midrin, Migratine, Migrin-A


Chemical Class: Sympathomimetic amine

image Clinical Pharmacology:


Mechanism of Action: Acetaminophen: A central analgesic whose exact mechanism is unknown, but appears to inhibit prostaglandin synthesis in the CNS and, to a lesser extent, block pain impulses through peripheral action. Acetaminophen acts centrally on hypothalamic heat-regulating center, producing peripheral vasodilation (heat loss, skin erythema, sweating). Isometheptene: An indirect-acting sympathomimetic agent with vasoconstricting activity whose exact mechanism is unknown, but appears to constrict cerebral blood vessels and reduce pulsation in cerebral arteries that may be responsible for the pain of migraine headaches. Dichloralphenazone: A complex of chloral hydrate and antipyrine that acts as a mild sedative and relaxant. Therapeutic Effect: Relieves migraine headaches.

Pharmacokinetics: Rapidly, completely absorbed from GI tract; rectal absorption variable. Widely distributed to most body tissues. Acetaminophen is metabolized in liver; excreted in urine. Dichloralphenazone is hydrolyzed to active compounds chloral hydrate and antipyrine. Chloral hydrate is metabolized in the liver and erythrocytes to the active metabolite trichloroethanol, which may be further metabolized to inactive metabolite. It is also metabolized in the liver and kidneys to inactive metabolites. The pharmacokinetics of isometheptene is not reported. Removed by hemodialysis. Half-life: Acetaminophen: 1-4 hr (half-life is increased in those with liver disease, elderly, neonates; decreased in children).

image Available Forms:


• Capsules: Acetaminophen 325 mg, isometheptene mucate 65 mg, dichloralphenazone 100 mg (I.D.A, Midrin, Migrin-A).

image Indications and Dosages:


Migraine headache: PO Initially, 2 capsules, followed by 1 capsule every hour until relief is obtained. Maximum: 5 capsules/12 hr.

Tension headache: PO 1-2 capsules q4h. Maximum: 8 capsules/24 hr.

image Contraindications: Glaucoma, hypersensitivity to acetaminophen, isometheptene, dichloralphenazone, or any component of the formulation, hepatic disease, hypertension, organic heart disease, MAO inhibitor therapy, severe renal disease



image Side Effects



Occasional

Transient dizziness

Rare

Hypersensitivity reaction


image Serious Reactions



• Acetaminophen toxicity is the primary serious reaction.

• Early signs and symptoms of acetaminophen toxicity include anorexia, nausea, diaphoresis, and generalized weakness within the first 12 to 24 hr.

• Later signs of acetaminophen toxicity include vomiting, right upper quadrant tenderness, and elevated liver function tests within 48 to 72 hr after ingestion.

• The antidote to acetaminophen toxicity is acetylcysteine.

image Geriatric side effects at a glance:


image CNS

image Bowel Dysfunction

image Bladder Dysfunction

image Falls


image U.S. Regulatory Considerations



image FDA Black Box

image OBRA regulated in U.S. Long Term Care


acetazolamide


(a-seat-a-zole’-a-mide)


image Brand Name(s): Dazamide, Diamox, Diamox Sequels


Chemical Class: Carbonic anhydrase inhibitor; sulfonamide derivative

image Clinical Pharmacology:


Mechanism of Action:

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Jun 8, 2016 | Posted by in GERIATRICS | Comments Off on A

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