Phentolamine (Mesylate)

Drug #566

Phentolamine (Mesylate) is alpha-adrenoceptor blocking drug with partial agonist and smooth muscle relaxant activity . Phentolamine (Mesylate) is used in the management of hypertension associated with pheochromocytoma, also used as a diagnostic test.

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Primary Characteristics

It is of Synthetic origin and belongs to Imidazole.

It belongs to Alpha adrenergic antagonist pharmacological group on the basis of mechanism of action and also classified in Antihypertensive Agents pharmacological group.

Molecular Weight: 377.5 · pK_a: 7.7 · Solubility in Water: 1 in 1 · Solubility in Alcohol: 1 in 5 · Non-proprietary name: Phentolamine (Mesylate) · pH: 3.5 · Isotonic value: 8.23.

Molecular structure of Phentolamine (Mesylate)

Pharmacokinetics

Absorption: Phentolamine (Mesylate) has an oral bioavailability is 45.5% (±4.5%).

Distribution: Phentolamine (Mesylate) has a plasma protein binding is 54 %.

Elimination: plasma half-life is 90 min, renal excretion is 70 %.

Indications

Phentolamine (Mesylate) is primarily indicated in conditions like Hypertension, Impotency, Phaeochromocytoma, Prophylaxis of NSAID-induced ulcer.

Phentolamine (Mesylate) is also indicated for secondary conditions like Skin necrosis.

Contraindications

Phentolamine (Mesylate) is contraindicated in conditions like Hypotension, Obstructive cardiomyopathy, Cardiovascular disease, Cerebrovascular disease, Aortic stenosis.

Dosage

Phentolamine (Mesylate)'s dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0.071 mg/kg	0.071 mg/kg	—	IM	As Required
0.071 mg/kg	0.071 mg/kg	—	IV	As Required
Paediatric Dosage (20kg)
0.3 mg/kg	0.3 mg/kg	—	Intra Venous	Single Dose, As Required
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown5 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Phentolamine (Mesylate) produces potentially life-threatening effects which include Hypotension. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Phentolamine (Mesylate) are Hypotension, Tachycardia , Cardiac arrhythmias, Headache, Excitation , Sweating , Visual distrubances, Hypoglycemia.

Phentolamine (Mesylate) is known to cause more or less tolerable side effects which are usually transient. These include Diarrhea, Nausea and vomiting.

Warnings / Precautions

Phentolamine should not be given to patients with angina pectoris, ischaemic heart disease. Care should be taken in patients with peptic ulcer disease.

Interference in Pathology

Phentolamine (Mesylate) may interfere in the diagnosis of Colorimetric measurement of 5-OH-Indoleaceticacid,false high values .

Available Brands

None recorded.

Storage Conditions

Phentolamine (Mesylate) should be stored Inj.

Drug Classification

1.12.3.5 — Alpha-1 receptor antagonists