Dapoxetine


Concise Prescribing Info
Indications/Uses
Premature ejaculation.
Dosage/Direction for Use
Adult : PO 18-64 yr Initial: 30 mg approx 1-3 hr before sexual activity. Subsequent doses adjusted according to response. Max: 60 mg. Dose should not be taken more than once in 24 hr.
Dosage Details
Oral
Ejaculation, premature
Adult: 18-64 yr Initially, 30 mg approx 1-3 hr before sexual activity, subsequent doses adjusted according to response. Max: 60 mg. Dose should not be taken more than once in 24 hr. Review treatment after 4 wk (6 doses) and at least 6 mthly thereafter.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Moderate to severe: Contraindicated.
Administration
May be taken with or without food. Swallow tab whole & take w/ a full glass of water.
Contraindications
Significant cardiac disease, history of syncope or mania, bipolar disorder, severe depression. Severe renal and moderate to severe hepatic impairment. Concomitant use w/ potent CYP3A4 inhibitors. Not to be used w/ or w/in 14 days of discontinuing treatment w/ antidepressants including other SSRIs and serotonin norepinephrine reuptake inhibitors (SNRIs) or MAOIs.
Special Precautions
Patient w/ bleeding disorders, epilepsy, susceptibility to angle-closure glaucoma or raised intraocular pressure. Not intended for use in women. Known CYP2D6 poor metabolisers.
Adverse Reactions
Nausea, vomiting, diarrhoea, constipation, abdominal pain or distension, dyspepsia, dry mouth, flushing, sweating, HTN, malaise, irritability, dizziness, headache, anxiety, agitation, abnormal dreams, sleep disturbances, drowsiness, tremor, paraesthesia, impaired attention, sexual dysfunction, visual disturbances, tinnitus.
Patient Counseling Information
May impair ability to drive and operate machinery.
Overdosage
Symptoms: Somnolence, GI disturbances (e.g. nausea, vomiting), tachycardia, tremor, agitation and dizziness. Management: Symptomatic and supportive treatment.
Drug Interactions
Concomitant use w/ PDE-5 inhibitors may result in orthostatic hypotension. Significant increase in exposure w/ moderate CYP3A4 inhibitors (e.g. fluconazole, verapamil) or potent CYP2D6 inhibitors (e.g. fluoxetine).
Potentially Fatal: Increased exposure w/ potent CYP3A4 inhibitors (e.g. ketoconazole, ritonavir, telithromycin). Concurrent use w/ SSRIs, SNRIs or MAOIs may increase the risk of serotonin associated effects. Prolonged QT interval w/ thioridazine.
Food Interaction
Avoid alcohol as it may increase neurocognitive and neurocardiogenic (e.g. syncope) adverse events, thereby increasing the risk of accidental injury. Increased risk of serotonin syndrome w/ St John’s wort.
Action
Description: Dapoxetine is a potent short-acting SSRI. Its action is assumed to be due to the inhibition of neuronal reuptake of serotonin and the subsequent potentiation of the neurotransmitter's action at pre- and postsynaptic receptors.
Pharmacokinetics:
Absorption: Rapidly absorbed. Absolute bioavailability: 42%. Time to peak plasma concentration: Approx 1-2 hr.
Distribution: Volume of distribution: 162 L. Plasma protein binding: <99%.
Metabolism: Extensively metabolised to multiple metabolites primarily through N-oxidation, N-demethylation, naphthyl hydroxylation, glucuronidation and sulfation.
Excretion: Via urine as conjugates. Terminal half-life: Approx 19 hr.
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Dapoxetine, CID=71353, https://pubchem.ncbi.nlm.nih.gov/compound/Dapoxetine (accessed on Jan. 20, 2020)

References
Buckingham R (ed). Dapoxetine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/08/2014.

Joint Formulary Committee. Dapoxetine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/08/2014.

Disclaimer: This information is independently developed by MIMS based on Dapoxetine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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