Trade Names:Ismelin- Tablets 10 mg- Tablets 25 mg
Interferes with release or distribution of norepinephrine from nerve endings, resulting in reduction in total peripheral resistance and diastolic and systolic BP.
Converted by the liver to 3 metabolites that are less active than the parent drug.
Renal Cl is 56 mL/min. T 1/ 2 is 1.5 to 8 d. Renal excretion.
Treatment of moderate and severe hypertension and renal hypertension, including that secondary to pyelonephritis, renal amyloidosis, and renal artery stenosis.
Reflex sympathetic dystrophy and causalgia.
Known or suspected pheochromocytoma; frank CHF not related to hypertension; use of MAOIs.
PO 10 mg every day initially; may increase by about 10 mg at 5 to 7 days; increase only if no decrease in standing BP is observed. Maintenance dose: 25 to 50 mg every day.Hospitalized
PO 25 to 50 mg initially; increase by 25 or 50 mg/day or every other day until desired response is obtained. Loading dose (for severe hypertension): Give at 6 h intervals over 1 to 3 days, omitting nighttime dose.Children
PO 0.2 mg/kg/24 h (6 mg/m 2 /24 h) as single oral dose initially; increase by increment of 0.2 mg/kg/24 h every 7 to 10 days. Max: 3 mg/kg/24 h.
Store in tightly closed container at room temperature.
May reverse hypotensive effect of drug.MAOIs
May decrease effectiveness of guanethidine; discontinue MAOIs more than 1 wk before starting guanethidine therapy.Phenothiazines
May inhibit hypotensive effect.Sympathomimetics (eg, ephedrine, epinephrine)
May reverse hypotensive effect of guanethidine; guanethidine may potentiate effects of sympathomimetics.Tricyclic antidepressants
May inhibit hypotensive effect of drug.
None well documented.
Bradycardia; orthostatic fluid retention; edema; angina.
Dizziness; weakness; lassitude; syncope; fatigue; muscle tremor; mental depression; chest paresthesias; ptosis; headache; confusion.
Blurred vision; nasal congestion.
Nausea; vomiting; dry mouth; parotid tenderness; diarrhea (may be severe, requiring discontinuation of therapy); increase in bowel movements.
Inhibition of ejaculation; nocturia; urinary incontinence; priapism.
Dyspnea; asthma in susceptible individuals.
Myalgia; weight gain; dermatitis; scalp hair loss; leg cramps.
Category C .
Excreted in breast milk.
Safety and efficacy not established.
More prone to side reactions of guanethidine therapy, especially orthostatic hypotension.
Use very cautiously, because hypotension may worsen renal function impairment.
May aggravate the hypersensitive condition of asthmatics because of further catecholamine depletion.
Use cautiously in patients with coronary disease, recent MI, or cerebral vascular disease, especially with encephalopathy; avoid use in patients with severe cardiac failure.
May decrease dosage requirements.
Occurs frequently, especially during initial treatment and with postural changes.
Ulcers may be aggravated by relative increase in parasympathetic tone.
Withdrawal is recommended 2 wk prior to surgery to reduce risk of vascular collapse and cardiac arrest during anesthesia; during emergency surgery administer preanesthetic and anesthetic agents cautiously in reduced dosages and prepare for possible vascular collapse.
Severe drowsiness, hypotension, bradycardia, severe diarrhea, nausea, vomiting, syncope.
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