TIGER MAN 5
Therapeutic Category:Urinary tract drugs
Pharmacologic Category:Phosphodiesterase-5 Enzyme Inhibitor
Composition:Vardenafil Hydrochloride 5mg
Film Coated Tablets
Penile erection is a hemodynamic process initiated by releasing NO. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) producing relaxation of smooth muscle in the corpus cavernosum and its associated arterioles.
Vardenafil inhibits the PDE5 which is responsible of cGMP degradationin the corpus cavernosum.
When the sexual stimulation causes NO release Vardenafil inhibits PDE5 consequently increases cGMP levels in the corpus cavernosum, resulting in smooth muscle relaxation and blood flow.
Vardenafil has no effect in the absence of sexual stimulation.
The inhibitory effect of Vardenafil is more selective on PDE5 than for other known phosphodiesterases.
Vardenafil is rapidly absorbed with absolute bioavailability of approximately 15%. Maximum observed plasma concentrations after a single 20 mg dose in healthy volunteers are usually reached between 30 minutes and 2 hours.
Vardenafil and its major circulating metabolite, M1, are highly bound to plasma proteins.
Vardenafil is metabolized predominantly by the hepatic enzyme CYP3A4.The major circulating metabolite, M1, results from desethylation at the piperazine moiety of Vardenafil. This metabolite shows a phosphodiesterase selectivity profile similar to that of Vardenafil.
After oral administration, Vardenafil is excreted as metabolites predominantly in the feces (approximately 91-95%) and to a lesser extent in the urine.
TIGERMAN is indicated for the treatment of erectile dysfunction.
- TIGERMAN is contraindicated for patients with a known hypersensitivity to any component of the tablet.
- Administration of TIGERMAN with nitrates and nitric oxide donors is contraindicated.
4-WARNINGS & PRECAUTIONS:
- The evaluation of erectile dysfunction should include a determination of potential underlying causes, a medical assessment, and the identification of appropriate treatment.
- Caution should be taken about cardiovascular status due to the potential cardiac risk of sexual activity for patients with preexisting cardiovascular risk factors.
- Caution should be taken when treating patients with bleeding disorders or significant active peptic ulceration.
- Treatment for erectile dysfunction should generally be used with caution by patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis, or Peyronie's disease) or by patients who have conditions that may predispose them to priapism (such as sickle cell anemia, multiple myeloma, or leukemia).
- The safety and efficacy of TIGERMAN used in combination with other treatments for erectile dysfunction have not been studied. So it is not recommended to use TIGERMAN in combination with other treatments for erectile dysfunction.
- Stop taking TIGERMAN and contact your doctor right away if you notice a sudden decrease or loss of hearing. Ringing in the ears and dizziness may also occur.
Effect of other drugs on TIGERMAN:
- When TIGERMAN combined with CYP3A4 inhibitors that results in AUC and Cmax increase consequently clearance decrease.
- When TIGERMAN is taken concomitantly with HIV Protease Inhibitors (Indinavir, Ritonavir) that obviously increases AUC and Cmax, it is recommended not to exceed a single 2.5 mg TIGERMAN dose in a 24hr period.
- There is no pharmacokinetic interactions were observed between vardenafil and the following drugs: Glyburide, Warfarin, Digoxin, Magnesium Hydroxide and Ranitidine.
Effect of TIGERMAN on other drugs:
- Vardinafil is contraindicated in combination with nitrates.
- When Vardenafil is combined with Indinavir and Ritonavir that will increase their AUC and Cmax
- Vardenafil has no effect in prolong bleeding time when combined with aspirin.
- Taking Vardenafil concomitantly with alpha-blockers may cause hypotension and syncope. Concomitant treatment should be initiated only if the patient is stable on his alpha blocker therapy, in those patient who are stable on alpha-blocker therapy, TIGERMAN should be initiated at the lowest recommended starting dose.
6-USE IN PREGNANCY, LACTATION AND PEDIATRICS:
Vardenafil is not indicated for women, children or neonates
Plasma concentration increases in males over 65 years, consequently 5 mg is recommended as starting dose.
The most common side effects: headache, flushing, sinusitis, dyspepsia, dizziness or nausea.
In rare cases the following side effects may appear: Anaphylactic reactions, asthenia, sudden decrease of hearing, chest pain, hypotension or hypertension, tachycardia, syncope, diarrhea, abdominal pain, dry mouth, neck and back pain, hypertonia, insomnia, apnea, pharyngitis, abnormal or blurred vision, rash and photosensitivity reactions, abnormal ejaculation and priapism.
9-DOSAGE & ADMINISTRATION:
- The usual initial dose is 10 mg administered orally about 60 minutes before sexual activity. The dose may be increased to 20 mg or reduced to 5 mg due to the resulting efficacy or side effects. The dose must be taken once daily. TIGERMAN can be taken regardless of food intake.Sexual stimulation is required for a natural response to treatment with TIGERMAN.
- Geriatric dose: The initial dose is 5 mg for males over 65 years old.
- In case of renal impairment the dose must not exceed 10 mg.
- TIGERMAN dose must be adjusted in case of concomitant use with potent CYP3A4 inhibitors: For ritonavir, a single dose of 2.5 mg TIGERMAN should not be exceeded in a 72-hour period. For Indinavir, Saquinavir, Atazanavir, Ketoconazole 400 mg and Clarithromycin, a single dose of 2.5 mg TIGERMAN should not be exceeded in a 24-hour period. For Ketoconazole 200 mg, Itraconazole, and Erythromycin, a single dose of 5 mg should not be exceeded in a 24-hour period.
- Concomitatnt treatment should be initiated only if the patient is stable on his alpha blocker therapy, in those patients who are stable on alpha-blocker therapy, TIGERMAN should be initiated at the lowest recommended starting dose which is 5 mg (2.5 mg when used concomitatntly with certain CYP3A4 inhibitors).
10-PACKAGING & COMPOSITION:
-TIGERMAN 5 - Film Coated Tablets: A pack of 4 or 10 film-coated tablets. Each film-coated tablet contains 5 mg of Vardenafil (HCl).
-TIGERMAN 10 - Film Coated Tablets: A pack of 4 or 10 film-coated tablets. Each film-coated tablet contains 10 mg of Vardenafil (HCl).
-TIGERMAN 20 - Film Coated Tablets: A pack of 4 or 10 film-coated tablets. Each film-coated tablet contains 20 mg of Vardenafil (HCl).
Store TIGERMAN - Film Coated Tablets at temperature between (20-25)°C.