Tadalafil; Uses, Dosage, Side Effects, Interaction ,Pregnancy

Tadalafil
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Tadalafil is a carboline-based compound with vasodilatory activity. Tadalafil selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase- (PDE-5)-mediated degradation of cGMP, which is found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis. Inhibition of cGMP degradation by tadalafil results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, and, so, prolonged penile erection.

Tadalafil is an orally adminstered drug used to treat male erectile dysfunction (impotence). It is marketed worldwide under the brand name Cialis. It is a phosphodiesterase 5 (PDE5) inhibitor. Tadalafil’s distinguishing pharmacologic feature is its longer half-life (17.5 hours) compared with Viagra and Levitra (4-5 hours). This longer half-life results in a longer duration of action and is, in part, responsible for the Cialis nickname of the “weekend pill.

Mechanism of Action of Tadalafil 

Tadalafil 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 flows into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by tadalafil enhances erectile function by increasing the amount of cGMP.This then activates the enzyme guanylate cyclase which results in increased levels of cyclic guanosine monophosphate (cGMP), leading to smooth muscle relaxation in the corpus cavernosum, resulting in increased inflow of blood and an erection. Tadalafil 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 tadalafil 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, tadalafil should not cause an erection.

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Indications of Tadalafil 

Therapeutic Indications

  • Used for the treatment of erectile dysfunction.
  • is indicated in adults for the treatment of pulmonary arterial hypertension (PAH) classified as WHO functional class II and III, to improve exercise capacity.
  • Efficacy has been shown in idiopathic PAH (IPAH) and in PAH related to collagen vascular disease.
  • Treatment of erectile dysfunction in adult males.
  • In order for tadalafil to be effective, sexual stimulation is required.CIALIS is not indicated for use by women.
  • Treatment of erectile dysfunction in adult males.
  • In order for tadalafil to be effective, sexual stimulation is required.
  • Treatment of the signs and symptoms of benign prostatic hyperplasia in adult males.
  • Tadalafil Mylan is not indicated for use by women.
  • Treatment of erectile dysfunction in adult males. In order for tadalafil to be effective, sexual stimulation is required.
  • Treatment of the signs and symptoms of benign prostatic hyperplasia in adult males.
  • Tadalafil Lilly is not indicated for use by women.
  • Talmanco is indicated in adults for the treatment of pulmonary arterial hypertension (PAH) classified as WHO functional class II and III, to improve exercise capacity.
  • Efficacy has been shown in idiopathic PAH (IPAH) and in PAH related to collagen vascular disease.

Contra – Indications of Tadalafil 

  • Multiple Myeloma
  • Leukemia
  • Sickle Cell Anemia
  • increased risk of bleeding due to clotting disorder
  • increased risk of bleeding
  • Alcohol Intoxication
  • Pigmentary Retinopathy
  • Hearing loss
  • Severe Uncontrolled High Blood Pressure
  • Unpredictable Severe Constricting Chest Pain
  • Narrowing of the Aortic Heart Valve
  • hypertrophic cardiomyopathy
  • Life-Threatening Irregular Heart Rhythm
  • Chronic Heart Failure
  • Stroke
  • abnormally low blood pressure
  • Ulcer from Stomach Acid
  • Liver Problems
  • Severe Renal Impairment
  • Mild to Moderate Kidney Impairment
  • Peyronie’s Disease
  • Bent Penis On Erection
  • Fibrous Tissue Formation in the Penis
  • Seizures
  • Severe Insufficiency of the Autonomic Nervous System
  • Eye Disease Caused by Blood Flow Problems
  • Restrictive Cardiomyopathy
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Dosage of Tadalafil 

Strengths: 2.5 mg, 5 mg; 10 mg; 20 mg;

Erectile Dysfunction

Use as needed for ED

  • Initial dose: 10 mg orally once a day, as needed, prior to sexual activity
  • Maintenance dose: 5 to 20 mg orally once a day, as needed, prior to sexual activity based on individual efficacy and tolerability

Once a day use for ED

  • Initial dose: 2.5 mg orally once a day at approximately the same time, without regard to timing of sexual activity
  • Maintenance dose: 2.5 to 5 mg orally once a day based on individual efficacy and tolerability.

Benign Prostatic Hyperplasia (BPH)

  • 5 mg orally once a day at approximately the same time, without regard to timing of sexual activity

Pulmonary Hypertension

  • 40 mg PO once daily; dividing dose for more frequent dosing is not recommended
  • Patients also taking ritonavir: 20 mg PO once daily initially for ≥1 week; may be increased to 40 mg/day on basis of tolerability
  • 40 mg orally once a day.

Benign Prostatic Hyperplasia

  • 5 mg orally once a day at approximately the same time

Concomitant administration with finasteride

  • 5 mg orally once a day at approximately the same time, for up to 26 weeks

Once daily use for ED and BPH

  • 5 mg orally once a day at approximately the same time, without regard to timing of sexual activity

Side Effects of Tadalafil 

The most common side effects of tadalafil are

Common

Serious

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Drug Interactions of Tadalafil 

Tadalafil may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Tadalafil 

FDA pregnancy Category B

Tell your doctor if you are pregnant or plan to become pregnant.This medication falls into category B. This medication is not used by women. Based on animal studies, tadalafil is not predicted to increase the risk of adverse developmental abnormalities in humans.Lactation

This medication is not used by women.

References

 

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