Kifaru Composition, Use, Dose, Side Effect

Kifaru is a drug for men. It makes man get a firm erection and sustain it longer. It comes in different strengths. It is made by Shalina Laboratories PVT. LTD., India.

Kifaru 100

Kifaru Composition

Kifaru 50 Composition

Each film coated tablet contains:

Sildenafil Citrate equivalent to Sildenafil 50 mg

Color: FD&C Blue

Excipients: Microcrystalline Cellulose, Calcium Hydrogen Phosphate (Anhydrous), Hydroxyl Cellulose, Stearate, Purified Talc, Colloidal Anhydrous silica, Croscarmellose Sodium, Maize Starch, Sodium Benzoate, Hypromellose, Titanium Dioxide, Macrogols.

Kifaru 100 Composition

Each film-coated tablet contains:

Sildenafil Citrate equivalent to Sildenafil 100mg

Color: Indigo Carmine

Excipients: Calcium Hydrogen Phosphate, Maize starch, Sodium Benzoate, Colloidal Anhydrous Silica, Croscarmellose Sodium, Purified Talc, Magnesium Stearate, Microcrystalline Cellulose, Hydroxypropyl cellulose, Hypromellose, Macrogols, titanium Dioxide.

Pharmacological Category

Kifaru Sildenafil Citrate is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).

Pharmacological Action

Kifaru has physiologic mechanism of action of the penis which involves release of nitric oxide in the corpus cavernosum during sexual stimulation. Nitric oxide then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP) producing smooth muscle relaxation in the corpus cavernosum and allowing inflow of blood. Kifaru has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of nitric oxide by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum.

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When sexual stimulation causes local release of nitric oxide, inhibition of PDE5 by sildenafil causes increased levels of cGMP in the corpus carvenosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. Sildenafil at recommended doses has no effect in the absence of sexual stimulation. Studies in vitro have shown that Kifaru is selective for PDE5.

Its effect is more potent on PDE5 than on other known phosphodiesterase (> 80-fold for PDE1, > 1,000-fold for PDE2, PDE3 and PDE4). The approximately 4000-fold selectivity for PDE5 versus PDE3 is important because PDE is involved in control of cardiac contractility. Kifaru is only 10-fold as potent for PDE5 compared to PDE6, an enzyme found in the retina; this lower selectivity is thought to be the basis for abnormalities related to color vision observed with higher doses or plasma levels.

The inhibition of PDE5 in these tissues by Kifaru may be the basis for the enhanced platelet antiaggregatory activity of nitric acid observed in vitro, an inhibition of platelet thrombus formation in vivo, and peripheral arterial venous dilatation in vivo.

Therapeutic indications Of Kifaru

Kifaru is used in the treatment of erectile dysfunction.

Contraindications

Kifaru was shown to potentiate the hypotensive effects of nitrates, and administration to patients who are using organic nitrates, either regularly and/or intermittent in any form, is therefore contraindicated. It is contraindicated in patients with a known hypersensitivity to any component of the preparation.

Dosage and Direction for Use Of Kifaru

The recommended dose is 50mg taken, as needed approximately 1 hour before sexual activity. However, Kifaru may be taken anywhere from hours to 0.5 hour before sexual activity. Based on effectiveness and toleration, the dose may be increased to a maximum recommended dose of 100mg or decreased to 25mg. The maximum recommended dosing frequency is once per day.

Pharmacokinetic Properties

Absorption: Rapidly absorbed.

Absolute Bioavailability: About 40%

Mean plasma concentration: 225ng/ml (Maximum absorption is within 30-absorption is within 30-120 minutes)

Terminal half-life: About 4 hours

Protein binding: About 96%

Elimination: Via feces and urine

Adverse Reaction

Long term use may cause allergic reactions, chest pain, angina pectoris, AV block, migraine, anemia, leukopenia, arthritis, tremor, asthma, skin ulcer, deafness, ear pain, urinary frequency, genital edema.

Undesirable Effects

Kifaru is generally well tolerated. Sometimes Kifaru causes headaches, flushing, dyspepsia, nasal congestion, abnormal vision, diarrhea, dizziness and rashes.

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Warnings And Precautions For Use In Special Populations

Cardiovascular effects: Carefully consider whether patients with certain underlying conditions (e.g., resting hypotension, fluid depletion) could be adversely affected by vasodilatory effects of sildenafil citrate. Not recommended in patients with pulmonary Veno-occlusive disease.

Use with alpha-blockers: Note additive blood pressure-lowering effects.

Bleeding: In patients with PAH secondary to CTD, higher rates of epistaxis with sildenafil citrate than placebo, including concomitant oral vitamin K antagonists.

Use with ritonavir and other potent CYP3A inhibitors: Coadministration not recommended.

Effects on the eye: Consider discontinuing sildenafil citrate if sudden loss of vision occurs, which could be non-arteritic anterior ischemic optic neuropathy (NAION).

Hearing impairment: Discontinue sildenafil citrate if sudden decrease or loss of hearing occurs.

Use with PDE5 inhibitors: Avoid use with Kifaru or other PDE5 inhibitors.

Prolonged erection: Advise patients to seek emergency treatment if an erection lasts > 4 hours. Use sildenafil citrate with caution in patients predisposed to priapism.

Pulmonary hypertension secondary to sickle cell disease: sildenafil citrate may cause serious Vaso-occlusive crises.

Renal Impairment: No dose adjustments required (including severe impairment CLcr < 30mL/min).

Hepatic Impairment: Mild to moderate require no dose adjustment. Severe has not been studied.

Geriatric: No data in 65 yrs. or older. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Usage in Pregnancy And Lactation: Not applicable as Kifaru is not indicated for women.

Use in nursing mothers: Not applicable as Kifaru is not indicated for women.

Effects on Ability to Drive and Operate Machinery: Not applicable.

Drugs Interaction

Cimetidine: Increases plasma concentrations of Kifaru.

Erythromycin: Increases AUC of Kifaru.

Ritonavir: Increases AUC and Cmax of Kifaru.

Saquinavir: Increases AUC and Cmax of Kifaru.

Rifampin: Decreases plasma levels of Kifaru.

Itraconazole Increases plasma levels of Kifaru.

Symptoms of over Dosage And its Treatment

In studies with healthy volunteers of single doses up to 800 mg, adverse events were similar to those seen at lower doses but rates and severities were increased. In cases of overdose, standard supportive measures should be adopted as required. Renal dialysis is not expected to accelerate clearance as sildenafil is highly bound to plasma proteins and it is not eliminated in the urine.