Vardenafil is a benzenesulfonamide derivative and phosphodiesterase type 5 (PDE5) inhibitor with vasodilatory activity. Vardenafil selectively inhibits PDE5, thus inhibiting the degradation of cyclic guanosine monophosphate (cGMP) found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis. The inhibition of cGMP degradation results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, prolonging penile erection.
Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection.
Mechanism of Action of Vardenafil
Vardenafil inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by vardenafil enhances erectile function by increasing the amount of cGMP.Vardenafil is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum. This means that, with vardenafil on board, normal sexual stimulation leads to increased levels of cGMP in the corpus cavernosum which leads to better erections. Without sexual stimulation and no activation of the NO/cGMP system, vardenafil should not cause an erection.
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Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMP-specific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP. Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 has no effect in the absence of sexual stimulation.
Indications of Vardenafil
- Erectile Dysfunction
- Black colour of panish & small size due to inadequate blood supply in panis
- Vardenafil relaxes muscles of the blood vessels and increases blood flow to particular areas of the body.
- Repair the cell of panish to strong enough in orgasom
- Poor sexual desire
- Poor control over intercourse
- Sexual Dysfunction,
- Persistent or recurrent ejaculation with minimal sexual stimulation before, on, or shortly after penetration and before the patient wishes; and
- Marked personal distress or interpersonal difficulty as a consequence of PE; and
- Poor control over ejaculation;
- A history of premature ejaculation in the majority of intercourse attempts over the prior 6 months.
- Very short sexual intercourse
- Sexual erectile dysfunction
- Inability to sustain a satisfactory erection to complete intercourse
Contra Indications of Vardenafil
- Multiple myeloma
- Leukemia
- Sickle cell anemia
- increased risk of bleeding due to clotting disorder
- Pigmentary retinopathy
- Hearing loss
- Severe uncontrolled high blood pressure
- Heart Attack
- Unpredictable severe constricting chest Pain
- Narrowing of the aortic heart valve
- hypertrophic cardiomyopathy
- prolonged QT interval on EKG
- Life threatening irregular heart rhythm
- Chronic heart failure
- Stroke
- abnormally low blood pressure
- Ulcer from stomach acid
- Severe liver disease
- Severe renal impairment
- Peyronie’s disease
- Bent penis on erection
- Fibrous tissue formation in the penis
- Eye disease caused by blood flow problems
Dosage of Vardenafil
Strengths : 2.5mg ,5mg ,10mg ,20mg
Erectile Dysfunction
- Adults—10 milligrams (mg) as a single dose, no more than once per day, approximately 1 hour before sexual activity.
- Adults 65 years and older—5 milligrams (mg) as a single dose, no more than once per day, approximately 1 hour before sexual activity. Your doctor may adjust your dose if needed. However, the dose is usually not more than 20 mg once per day.
- Adults up to 65 years—10 mg as a single dose, no more than once per day, approximately 1 hour before sexual activity. Your doctor may adjust your dose if needed. However, the dose is usually not more than 20 mg once per day.
- Children—Use is not recommended.
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Erectile Dysfunction
- Initial dose: 10 mg orally once a day, as needed, approximately 60 minutes before sexual activity. Increase to 20 mg or decrease to 5 mg based on efficacy and tolerability.
- Maximum dose: 20 mg once a day
- Initial dose: 5 mg orally once a day
Geriatric Erectile Dysfunction
65 years or older
- Initial dose: 5 mg orally once a day, as needed, approximately 60 minutes before sexual activity
Side Effects of Vardenafil
The most common
- Facial flushing (reddening),
- Headaches,
- Constipation
- sleepiness or unusual drowsiness
- clumsiness or unsteadiness
- dizziness
- drowsiness
- dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- Headache.
- Skin rashes.
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Serious
- agitation
- anxiety
- behavioral changes, including aggressiveness, angry outbursts, bizarre behavior, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- sleepwalking
Drug Interactions of Vardenafil
Vardenafil may interact with following drugs, supplements, & may change the efficacy of drugs
- alpha agonists (e.g., clonidine, methyldopa)
- alpha-blockers (e.g., doxazosin, terazosin)
- angiotensin converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
- angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
- aripiprazole
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- carbamazepine
- dexamethasone
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, )
- fusidic acid
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- methyldopa
- metronidazole
- phenytoin
- sertraline
- “statins” (e.g., lovastatin, simvastatin, atorvastatin)
- tocilizumab
- tyrosine kinase inhibitors (e.g., dasatinib, imatinib, nilotinib, sunitinib)
