Nefazodone (HCl)

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.

Brands
Adult Dose
Dose: 100 to 200 mg/day
Single Dose: 150 (150)
Frequency: 12 hourly
Route: PO
Instructions:
Neonatal
Paedriatic
Characteristics
Nefazodone (HCl) also known as Selective serotonin repptake inhibitors. . It is of Synthetic origin and belongs to Phenylpiperazine Analog. . The Molecular Weight of Nefazodone (HCl) is 506.50. Its pKa is 6.6.
Contraindications
Nefazodone (HCl) is contraindicated in conditions like Hypersensitivity,Lactation.
Effects
The severe or irreversible adverse effects of Nefazodone (HCl), which give rise to further complications include Hypomania, Serotonin syndrome.The signs and symptoms that are produced after the acute overdosage of Nefazodone (HCl) include Sinus bradycardia, Nausea & vomiting, Somnolence, Decreased systolic pressure.The symptomatic adverse reactions produced by Nefazodone (HCl) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Nausea, Fever, Constipation, Dry mouth, Blurred vision, Chills, Somnolence, Postural hypotension, Light headedness, Dry mouth, dizziness.
Indications
Nefazodone (HCl) is primarily indicated in conditions like Depression, Depressive illness.
Interactions
Nefazodone (HCl) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAstemizoleNefazodone increases the plasma concentration of astemizoleresults in increased level which may lead to prolonged QT interval, serious arrythmia and death.MajorThis combinition is considered contraindicated.DabrafenibStrong CYP3A4 inhibitors may increase levels of dabrafenibconsider alternate therapyDigoxinNefazodone may increase the serum concentration of Digoxin.ModerateMonitor for increased therapeutic effects of Digoxin if nefazodone is initiated/dose increased, or decreased effects if nefazodone is discontinued/dose decreased.ErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinibHaloperidolLeacance of Haloperidol is decreased by nefazodone.NaratriptanConcurrent use is not recommended, but dosages should be adjusted if concurrent use is required.NitrendipineMay increase the levels/effects of nitrendipine.PhenelzineRizatriptanConcurrent use may increase drowsiness.SalmeterolConcurrent use may potentiate the risk of cardiovascular adverse events.SunitinibMay increases sunitinib concentrations.TerfenadineNefazodone inhibit the metabolism of terfenadine.result in increased plasma concentration of terfenadine may lead to prolonged QT interval, arrythmia and death.MajorCoadministration of these agents is considered contraindicated.VemurafenibNefazodone inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.Vortioxetineincreases toxicity of vortioxetineuse alternative These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Tab Store Below 40°C.
Warnings
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.
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