Nefazodone (HCl)

Also known as: Selective serotonin repptake inhibitors

Drug #1549

Nefazodone (HCl) is a phenylpiperazine antidepressant structurally similar to trazodone, but nefazodone causes less sedation or orthostatic hypotension. Nefazodone is one of a new oral antidepressant with a mechanism of action distinct from other antidepressants. It blocks the reuptake of serotonin at presynaptic neurones and is an antagonist at post-synaptic 5-HT 2 receptors. It also inhibits reuptake of nor-adrenaline and blocks alpha-1 adrenoceptor but has no appearent effect on dopamine receptors. Nefazodone (HCl) is as effective as other antidepressants in treating major depression but lacks cardiovascular toxicity seen with tricyclics and does not cause restlessness or insomnia frequently associated with the selective serotonin reuptake inhibitors (SSRIs). Nefazodone was FDA approved in December 1994 for treatment of major depression.

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Primary Characteristics

Nefazodone (HCl) is also known as Selective serotonin repptake inhibitors.

It is of Synthetic origin and belongs to Phenylpiperazine Analog.

Molecular Weight: 506.5 · pK_a: 6.6 · Solubility in Water: 1 in 28 - 100 · Solubility in Alcohol: 1 in 25 · Non-proprietary name: Nefazodone (HCl).

Pharmacokinetics

Absorption: Nefazodone (HCl) has an oral bioavailability is 49.5% (±49.5%), pre-systemic (first-pass) metabolism accounts for 40% (±40%).

Distribution: Nefazodone (HCl) has a volume of distribution is 0.22 - 0.87 l/Kg. plasma protein binding is > 99 %.

Elimination: it is metabolised via Hepatic CYP3A4, plasma half-life is 6 hr, renal excretion is 49 - 65 %.

Indications

Nefazodone (HCl) is primarily indicated in conditions like Depression, Depressive illness.

Contraindications

Nefazodone (HCl) is contraindicated in conditions like Hypersensitivity, Lactation.

Dosage

Nefazodone (HCl)'s dosage details are as follows:

Dose	Single Dose	Frequency	Route
Adult Dosage
150 mg/day	150 mg/day	Every 12h	PO
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown1 interaction

11 interactions

Major2 interactions

Moderate1 interaction

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

Side Effects

Nefazodone (HCl) in overdosage may give rise to further complications which include Hypomania , Serotonin syndrome.

The signs and symptoms that are produced after acute overdosage of Nefazodone (HCl) are Sinus bradycardia, Nausea & vomiting, Somnolence, Decreased systolic pressure.

Nefazodone (HCl) is known to cause more or less tolerable side effects which are usually transient. These include Blurred vision, Chills, Constipation , Dizziness, Dry mouth, Fever, Light headedness, Nausea, Postural hypotension, Somnolence .

Warnings / Precautions

It should be used cautiously in patients with epilepys, a history of hypomania or mania, severe renal or hepatic impairment, and those with arecent history of myocardial infarction or unstable heart disease. It should be used with caution in cardiovascular or cerebrovascular diseases that could be exacerbated with hypotension, and in any condition such as dehydration or hypovolumia that may predispose patient to hypotension. Patients should not derived or operate machinary. The dose may be increased gradually. Elderly patients, especially females may have higher plasma concentration than other patients. Doses should be restricted to lower end of the range in patients with hepatic or severe renal impairment. Patient should be closely monitored during early antiderpressant therapy until improvement in depression is observed because suiside is an inherent risk in depressed pateints. It should be withdrawn gradually to reduce the risk of withdrawal symptoms.

Available Brands

None recorded.

Storage Conditions

Nefazodone (HCl) should be stored Tab.

Drug Classification

1.24.2.1 — Drugs used in depression