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phenoxybenzamine (Dibenzyline)

 

Classes: Alpha Blockers, Antihypertensives

Dosing and uses of Dibenzyline (phenoxybenzamine)

 

Adult dosage forms and strengths

capsule

  • 10mg

 

Hypertension Pheochromocytoma

10 mg PO BID initially; increase qOD to 20-40 mg PO BID/TID (sometimes higher doses necessary)

 

Bladder Management (Off-label)

Initial 10 mg PO qD; can be increased q5d by 10 mg PO q8-12hr

 

Other Indications & Uses

Off-label: Raynaud's phenomenon, overactive bladder (neurogenic, prostatic obstruction), shock, hypertensive emergencies d/t epinephrine

 

Pediatric dosage forms and strengths

capsule

  • 10mg

 

Pheochromocytoma Hypertension (Off-label)

0.25-1 mg/kg PO qD; increase to effect slowly; not to exceed 10 mg/day

 

Dibenzyline (phenoxybenzamine) adverse (side) effects

Frequency not defined

Orthostatic hypotension

Tachycardia

Dizziness

Drowsiness

Fatigue

Malaise

Sedation

Dry mouth

Nausea

Vomiting

Inhibition of ejaculation

Miosis

Nasal congestion

 

Warnings

Contraindications

Hypersensitivity to phenoxybenzamine

Any conditions in which fall in BP is undesirable

Orthostatic hypotension

 

Cautions

Cerebral or coronary arteriosclerosis, CHF, respiratory infection, renal impairment

Concomitant use of drugs that stimulate alpha/beta receptors (may incr hypotension/tachycardia)

May have carcinogenic potentiaL

First dose effect may occur, causing a sudden and drastic fall in blood pressure after administering the first dose.

Hypotension/syncope may occur with first few doses or with increase in dose

Minimize by using small first dose at bedtime

Increase dose slowly

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Not known if excreted into breast milk, discontinue drug or do not nurse

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Dibenzyline (phenoxybenzamine)

Half-Life: 24 hr

Onset: several hours

Duration: several days

Bioavailability: 20-30%

Metabolism: extensively metabolized in liver

Metabolite: N-phenoxyisopropyl-benzylamine

Excretion: urine & feces

 

Mechanism of action

Alpha blocker, noncompetitive alpha-adrenergic blockade of post ganglionic synapses in smooth muscle, exocrine glands