E
econazole nitrate
Brand Name(s): Spectazole
Clinical Pharmacology:Mechanism of Action: An imidazole derivative that changes the permeability of the fungal cell wall. Therapeutic Effect: Inhibits fungal biosynthesis of triglycerides, phospholipids. Fungistatic.
Pharmacokinetics: Low systemic absorption. Protein binding: 98%. Metabolized in liver to more than 20 metabolites. Primarily excreted in urine; minimal excretion in feces. Not removed by hemodialysis.
Available Forms:
Indications and Dosages:Treatment of tinea pedis, tinea cruris, tinea corporis, tinea versicolor: Topical Apply once daily to affected area for 2-4 wk.
Unlabeled Uses: Cutaneous candidiasis, otomycosis
Contraindications: Hypersensitivity to econazole
Side Effects
Serious Reactions
Patient/Family Education
• For external use only; avoid contact with eyes; cleanse skin with soap and water and dry thoroughly prior to application
• Use medication for full treatment time outlined by clinician, even though symptoms may have improved
Monitoring Parameters
Geriatric side effects at a glance:
U.S. Regulatory Considerations
edetate calcium disodium (calcium EDTA)
(ed’-eh-tate kal’-see-um dye-soe’-dee-um)
Brand Name(s): Calcium Disodium Versenate
Clinical Pharmacology:Mechanism of Action: A chelating agent that reduces blood concentration of heavy metals, especially lead, forming stable complexes. Therapeutic Effect: Allows heavy metal excretion in urine.
Pharmacokinetics: Well absorbed after parenteral administration; poorly absorbed from the gastrointestinal (GI) tract. Penetrates to extracellular fluid and slowly diffuses into cerebrospinal fluid (CSF). No metabolism occurs. Excreted in the urine either unchanged or as the metal chelates. Half-life: 20-60 min (IV), 1.5 hr (IM).
Available Forms:
Indications and Dosages:Diagnosis of lead poisoning: IM, IV 500 mg/m2. Maximum: 1 g/m2/day divided in equal doses 8-12 hr apart for 5 days, skip 2-4 days and repeat course if needed.
Lead poisoning (without encephalopathy): IM/IV 1-1.5 g/m2 daily for 3-5 days (if blood lead concentration >100 mcg/dl, calcium edetate usually given with dimercaprol.) Allow at least 2-4 days, up to 2-3 wk between courses of therapy. Patients should not be given more than 2 courses of therapy.
Lead poisoning (with encephalopathy): IM Initially, dimercaprol 4 mg/kg; then give dimercaprol 4 mg/kg and calcium EDTA 250 mg/m2; then 4 hr later and q4h for 5 days.
Contraindications: Anuria, severe renal disease, hypersensitivity to EDTA or any component of the formulation
Side Effects
Chills, fever, anorexia, headache, histamine-like reaction (sneezing, stuffy nose, watery eyes), decreased BP, nausea, vomiting, thrombophlebitis
Serious Reactions
Patient/Family Education
Monitoring Parameters
• Urinalysis and urine sediment daily during therapy to detect signs of progressive renal tubular damage
• Renal function tests, liver function tests, and serum electrolytes before and periodically during therapy
Geriatric side effects at a glance:
U.S. Regulatory Considerations
FDA Black Box
edetate disodium
Brand Name(s): Disotate, Endrate
Clinical Pharmacology:Mechanism of Action: A chelating agent that forms a soluble chelate with calcium, resulting in rapid decrease in plasma calcium concentrations. Therapeutic Effect: Allows calcium to be excreted in urine.
Pharmacokinetics: Distributed in extracellular fluid and does not appear in red blood cells. No metabolism occurs. Rapidly excreted in the urine. Half-life: 1.4-3 hr.
Available Forms:
Indications and Dosages:Digitalis toxicity, hypercalcemia: IV 500 mg/kg/day over 3 hr or more, daily for 5 days, skip 2 days, repeat as needed up to 15 doses. Maximum: 3 g/day.
Contraindications: Anuria, renal impairment, hypersensitivity to EDTA or any component of the formulation
Side Effects
Abdominal cramps or pain, diarrhea, nausea, vomiting, circumoral paresthesia, headache, numbness, postural hypotension
Serious ReactionsSpecial Considerations
• Have patient remain supine for a short time after INF due to the possibility of orthostatic hypotension
Monitoring Parameters
Geriatric side effects at a glance:
U.S. Regulatory Considerations
FDA Black Box
edrophonium chloride
(ed-roe-foe’-nee-um klor’-ide)
Brand Name(s): Enlon, Reversol, Tensilon
Clinical Pharmacology:Mechanism of Action: A parasympathetic, anticholinesterase agent that inhibits destruction of acetylcholine by acetylcholinesterase, thus causing accumulation of acetylcholine at cholinergic synapses. Results in an increase in cholinergic responses such as miosis, increased tonus of intestinal and skeletal muscles, bronchial and ureteral constriction, bradycardia, and increased salivary and sweat gland secretions.
Pharmacokinetics: Onset of action occurs within 30-60 sec and has duration of 10 min. Rapid absorption after IV administration. Exact method of metabolism is unknown. Rapidly excreted in urine. Half-life: 1.8 hr.
Available Forms:
Indications and Dosages:Diagnosis of myasthenia gravis: IV 2-mg test dose over 15-30 sec. If no reaction in 45 sec, give additional dose of 8 mg. Test dose may be repeated after 30 min. IM/SC Initially, 10 mg as a single dose. If no cholinergic reaction occurs, give 2 mg 30 minutes later to rule out false-negative reaction.
Neuromuscular blockade antagonism: IV 10 mg over 30-45 sec. May be repeated as needed until a cholinergic response is detected. Maximum: 40 mg.
Contraindications: Gastrointestinal (GI) or genitourinary (GU) obstruction, hypersensitivity to edrophonium, sulfites, or any component of the formulation
Side Effects
Increase salivation, intestinal secretions, lacrimation, urinary urgency, hyperperistalsis, sweating
Serious Reactions
Patient/Family Education
• Notify the physician or health care advisor of difficulty breathing, dizziness, muscle cramps and spasms, or vomiting
Monitoring Parameters
Geriatric side effects at a glance:
U.S. Regulatory Considerations
efalizumab
Brand Name(s): Raptiva
Clinical Pharmacology:Mechanism of Action: A monoclonal antibody that interferes with lymphocyte activation by binding to the lymphocyte antigen, inhibiting the adhesion of leukocytes to other cell types. Therapeutic Effect: Prevents the release of cytokines and the growth and migration of circulating total lymphocytes, predominant in psoriatic lesions.
Pharmacokinetics: Clearance is affected by body weight, not by gender or race, after subcutaneous injection. Serum concentration reaches steady state at 4 wk. Mean time to elimination: 25 days.
Available Forms:
Indications and Dosages:Psoriasis: Subcutaneous Initially, 0.7 mg/kg followed by weekly doses of 1 mg/kg. Maximum: 200 mg (single dose).
Contraindications: Concurrent use of immunosuppressive agents, hypersensitivity to any murine or humanized monoclonal antibody preparation
Side Effects
Serious Reactions
Patient/Family Education
• Intended for use under the guidance and supervision of clinician; patients may self-inject if appropriate and with medical follow-up, after proper training in injection technique, including proper syringe and needle disposal
• Notify the health care provider if bleeding from the gums, bruising or petechiae of the skin, or signs of infection occur
Monitoring Parameters
• Efficacy: Improvement of clinical signs/symptoms of psoriasis (e.g., itching, redness, scaling, psoriatic body surface area coverage); PASI scores are based on plaque thickness, scaling, and redness, adjusted for percentage of affected body surface area; quality of life assessments
• Toxicity: CBC with differential periodically, particularly platelets; vital signs in patients with a history of hypersensitivity to any medication (first injection); temperature periodically (infection)
Geriatric side effects at a glance:
U.S. Regulatory Considerations
efavirenz
Brand Name(s): Sustiva
Clinical Pharmacology:Mechanism of Action: A non-nucleoside reverse transcriptase inhibitor that inhibits the activity of HIV reverse transcriptase of HIV-1 and the transcription of HIV-1 RNA to DNA. Therapeutic Effect: Interrupts HIV replication, slowing the progression of HIV infection.
Pharmacokinetics: Rapidly absorbed after PO administration. Protein binding: 99%. Metabolized to major isoenzymes in the liver. Eliminated in urine and feces. Half-life: 40-55 hr.
Available Forms:
Indications and Dosages:
Contraindications: Concurrent use with ergot derivatives, midazolam, or triazolam; efavirenz as monotherapy
Side Effects
Mild to severe: Dizziness, vivid dreams, insomnia, confusion, impaired concentration, amnesia, agitation, depersonalization, hallucinations, euphoria, somnolence (mild symptoms don’t interfere with daily activities; severe symptoms interrupt daily activities)
Serious Reactions
Patient/Family Education
• May be taken without regard for meals; absorption increased by a high-fat meal, which should be avoided
Monitoring Parameters
• Monitor the patient for adverse CNS and psychological effects, such as abnormal dreams, dizziness, impaired concentration, insomnia, severe acute depression (including suicidal ideation or attempts), and somnolence. Be aware that insomnia may begin during the first or second day of therapy and generally resolves in 2-4 wk
Geriatric side effects at a glance:
U.S. Regulatory Considerations
eflornithine
Brand Name(s): Vaniqa
Clinical Pharmacology:Mechanism of Action: A topical antiprotozoal that inhibits ornithine decarboxylase cell division and synthetic function in the skin. Therapeutic Effect: Reduces rate of hair growth.
Pharmacokinetics: Absorption is less than 1% from intact skin. Not metabolized. Primarily excreted as unchanged drug in urine. Half life: 8 hr.
Available Forms:
Indications and Dosages:For reduction of unwanted facial hair in women: Topical Apply thin layer to affected area of face and adjacent involved areas under chin; rub in thoroughly. Use twice daily at least 8 hr apart. Do not wash area for at least 4 hr.
Contraindications: Hypersensitivity to eflornithine or any component of the formulation
Side Effects
Serious ReactionsSpecial Considerations
• The most frequent, serious, toxic effect of eflornithine is myelosuppression, which may be unavoidable if successful treatment is to be completed; decisions to modify dosage or to interrupt or cease treatment depend on the severity of the observed adverse event(s) and the availability of support facilities
Patient/Family Education
Monitoring Parameters
• CBC with platelets before and twice weekly during therapy and qwk after completion of therapy until hematologic values return to baseline levels
Geriatric side effects at a glance:
U.S. Regulatory Considerations
eletriptan
Brand Name(s): Relpax
Clinical Pharmacology:Mechanism of Action: A serotonin receptor agonist that binds selectively to vascular receptors, producing a vasoconstrictive effect on cranial blood vessels. Therapeutic Effect: Relieves migraine headache.
Pharmacokinetics: Well absorbed after PO administration. Metabolized by the liver to inactive metabolite. Eliminated in urine. Half-life: 4.4 hr (increased in hepatic impairment and the elderly (older than 65 yr).
Available Forms:
Indications and Dosages:Acute migraine headache: PO 20-40 mg. If headache improves but then returns, dose may be repeated after 2 hr. Maximum: 80 mg/day.
Contraindications: Arrhythmias associated with conduction disorders, cerebrovascular syndrome including strokes and transient ischemic attacks (TIAs), coronary artery disease, hemiplegic or basilar migraine, ischemic heart disease, peripheral vascular disease including ischemic bowel disease, severe hepatic impairment, uncontrolled hypertension, use within 24 hr of treatment with another 5-HTd1 agonist, an ergotamine-containing or ergot-type medication such as dihydroergotamine (DHE) or methysergide
Side Effects
Serious Reactions
• Cardiac reactions (including ischemia, coronary artery vasospasm, and MI) and noncardiac vasospasm-related reactions (such as hemorrhage and cerebrovascular accident [CVA]) occur rarely, particularly in patients with hypertension, diabetes, or a strong family history of coronary artery disease; obese patients; smokers.
Patient/Family Education
• Avoid tasks that require mental alertness or motor skills until response to the drug has been established
• Notify the physician immediately if palpitations, pain or tightness in the chest or throat, pain or weakness in the extremities, or sudden or severe abdominal pain occurs
Monitoring Parameters
• Efficacy: Headache response 1-4 hr after a dose (reduction from moderate or severe pain to minimal or no pain); headache recurrence within 24 hr
• Toxicity: Vital signs (pulse, blood pressure), electrocardiogram, particularly in patient with coronary artery disease risk factors
Geriatric side effects at a glance:
U.S. Regulatory Considerations
Brand Name(s): Emtriva
Clinical Pharmacology:
