Ketanserin (Tartrate)

Drug #769

Chemically Ketanserin (Tartrate) is (+)-3-[2-[4-fluorobenzoyl)-1-piperidinyl]-2, 4 [1H, 3H]-quinazoline-dione. Ketanserin (Tartrate) is prepared by chemical synthesis and the dextrorotatary stereoisomer is used clinically. Ketanserin (Tartrate) is a serotonin antagonist with a high affinity for peripheral serotonin-2 (5-HT-2) receptors and thus inhibits serotonin-induced vasoconstriction, bronchoconstriction and platelet aggregation.it has also some a-1 antagonist and histamine H-1antagonist properties, but the clinical significance of these is controversial. Ketanserin is used in the management of hypertension and has also been tried in a variety of other conditions.

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Primary Characteristics

It is of Synthetic origin and belongs to 2.4(1h,3h) Quinazolivedione.

It belongs to 5HT-2 + alpha adrenergic antagonist pharmacological group on the basis of mechanism of action and also classified in Antihypertensive Agents pharmacological group. It is also classified under Psychotherapeutic Drugs .

Molecular Weight: 545.52 · pK_a: 7.5 · Solubility in Water: 1 in 42 · Solubility in Alcohol: 1 in 417 · Non-proprietary name: Ketanserin (Tartrate).

Molecular structure of Ketanserin (Tartrate)

Pharmacokinetics

Absorption: Ketanserin (Tartrate) has an oral bioavailability is 50% (±50%), pre-systemic (first-pass) metabolism accounts for 25% (±25%).

Distribution: Ketanserin (Tartrate) has a volume of distribution is 3-6 l/kg. plasma protein binding is 95%.

Elimination: it is metabolised via Hepatic (extensively), plasma half-life is 10-18 hr, renal excretion is 68%.

Indications

Ketanserin (Tartrate) is primarily indicated in conditions like Acute hypertensive episodes, Essential hypertension.

Ketanserin (Tartrate) is also indicated for secondary conditions like Bronchospasm, Vasodilator.

Contraindications

Ketanserin (Tartrate) is contraindicated in conditions like Hypersensitivity to any component of product.

Dosage

Ketanserin (Tartrate)'s dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
40 mg	40 mg	—
0.142 mg/kg	0.142 mg/kg	—	IM	Every 15-30 minutes, As Required
0.235 mg/kg.min	0.235 mg/kg.min	—	IV Inf	As Required
20 mg	20 mg	Every 12h	PO	For 2-4 weeks
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

None recorded.

Side Effects

Ketanserin (Tartrate) in overdosage may give rise to further complications which include Ventricular tachycardia .

Ketanserin (Tartrate) produces potentially life-threatening effects which include Ventricular arrhythmias. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Ketanserin (Tartrate) are Drowsiness, Drowsiness, Visual distrubances, Syncope , Sleepiness.

Ketanserin (Tartrate) is known to cause more or less tolerable side effects which are usually transient. These include Dizziness, Drowsiness, Dry mouth, Fatigue, GI disturbance, Headache, Lack of concentration, Light headedness, Sedation .

Warnings / Precautions

Patients should observe caution while driving or performing other tasks requiring alertness, because it may cause drowsiness. Ketanserin should be used with caution in patients receiving antiarrhythmics or those with 2nd or 3rd degree A.V. block. Caution should be taken to avoid hypokalaemia in patients taken ketanserin with diuretics.

Available Brands

None recorded.

Storage Conditions

Ketanserin (Tartrate) should be stored .

Drug Classification

1.12.8 — Other cardiovascular preparations