Dwafil 10
Pharmacodynamic properties:-
Tadalafil is a potent, selective, reversible inhibitor of cyclic guanosine
monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).
When sexual stimulation causes the local release of nitric oxide,
inhibition of PDE5 by Tadalafil produces increased levels of cGMP in
the corpus cavernosum. This results in smooth muscle relaxation and
inflow of blood into the penile tissues, thereby producing an erection.
Tadalafil has no effect in the absence of sexual stimulation.
Tadalafil administered to healthy subjects produced no significant
difference compared to placebo in supine systolic and diastolic blood
pressure, or in standing systolic and diastolic blood pressure, and no
significant change in heart rate.
There were no clinically relevant effects on sperm concentration, sperm
count, motility or morphology after daily doses of 10 mg and 20 mg
for 6 months.
Pharmacokinetic properties:-
- Tadalafil is readily absorbed after oral administration and the mean
maximum observed plasma concentration (Cmax) is achieved at a
median time of 2 hours after dosing.
- The rate and extent of absorption of tadalafil are not influenced by
food, thus Tadalafil may be taken with or without food. The time of
dosing (morning versus evening) had no clinically relevant effects on
the rate and extent of absorption.
- The mean volume of distribution is approximately 63 liters, indicating
that tadalafil is distributed into tissues. At therapeutic concentrations,
94% of Tadalafil in plasma is bound to proteins. Protein binding is not
affected by impaired renal function.
- Less than 0.0005% of the administered dose appeared in the semen of
healthy subjects.
- Tadalafil is predominantly metabolized by the cytochrome P450
(CYP3A4) isoform.
- The mean oral clearance for tadalafil is 2.5 L/hr and the mean half-life
is 17.5 hours in healthy subjects.
- Tadalafil is excreted predominantly as inactive metabolites, mainly in
the faeces (approximately 61% of the dose) and to a lesser extent in
the urine (approximately 36% of the dose).