Alyq (tadalafil)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tadalafil, a selective phosphodiesterase (PDE) type 5 inhibitor, is a vasodilating agent.
Tadalafil is a selective inhibitor of phosphodiesterases (PDEs), with the greatest selectivity for PDE type 5, the principal isoenzyme of PDE involved in the metabolism of cyclic guanosine monophosphate (cGMP) to GMP in the vascular smooth muscle, smooth muscle of the pulmonary vasculature, prostate, bladder, and corpora cavernosa of the penis. In patients with pulmonary hypertension, tadalafil induces relaxation of pulmonary vascular smooth muscle cells and vasodilation of the pulmonary vascular bed.
Tadalafil exhibits some activity against other phosphodiesterases. In vitro, tadalafil is >10,000-fold more potent for PDE type 5 than PDE type 1, PDE type 2, PDE type 4, and PDE type 7 enzymes, which are found in the heart, brain, blood vessels, liver, leukocytes, skeletal muscle, and other organs. Tadalafil is >10,000-fold more potent for PDE type 5 than for PDE type 3, an enzyme found in the heart and blood vessels.
Additionally, tadalafil is 700-fold more potent for PDE type 5 than for PDE type 6, which is found in the retina and is responsible for phototransduction.
Tadalafil is absorbed following oral administration; the absolute bioavailability has not been determined. The maximum observed plasma concentration is achieved between 2 and 8 hours (median time 4 hours). The rate and extent of absorption of tadalafil are not influenced by food, including a high-fat, high-calorie meal; thus tadalafil may be taken with or without food.
Tadalafil is distributed into tissues; at therapeutic concentrations the drug is 94% bound to proteins.
Tadalafil is predominantly metabolized in the liver by cytochrome P-450 (CYP) 3A4 to a catechol metabolite which undergoes extensive methylation and glucuronidation. In vitro data suggests that metabolites are not expected to be pharmacologically active at observed metabolite concentrations. Tadalafil is excreted principally as metabolites in the feces (61%) and urine (36%); the drug is not appreciably removed by hemodialysis.
The mean terminal half-life of tadalafil is 15 hours in healthy subjects. In patients with pulmonary arterial hypertension (PAH) not receiving concomitant bosentan, the mean terminal half-life of tadalafil is 35 hours. Tadalafil exposure (AUC) was reduced approximately 19% and peak plasma concentration reduced by 5% in male patients with diabetes mellitus compared to healthy subjects.
No clinically relevant differences in exposure to tadalafil have been identified in healthy female and male subjects or subjects from different ethnic groups.
USES: Tadalafil is used to treat high blood pressure in the lungs (pulmonary hypertension). It works by relaxing and widening the blood vessels in your lungs which allows the blood to flow more easily. Decreasing high blood pressure in the lungs allows your heart and lungs to work better and improves your ability to exercise.
Generic name: tadalafil
Pronunciation: (ta-DA-la-fil)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Alyq
Indications
The following indications are listed for Alyq:
- Pulmonary Arterial Hypertension
Also known as: Hypertensive Pulmonary Arterial Disease, Pulmonary Hypertensive Arterial Disease.
Dosing
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Tadalafil is metabolized principally via cytochrome P-450 (CYP) isoenzyme 3A4. Inhibitors and inducers of this isoenzyme may increase or decrease tadalafil exposure, respectively.
Tadalafil does not appear to induce or inhibit the clearance of other drugs metabolized by P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP), or CYP isoforms.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Concomitant use of organic nitrates or nitrites, either regularly or intermittently. Do not use nitrates within 48 hours of the last tadalafil dose.
*Concomitant use of guanylate cyclase stimulators (e.g., riociguat).
*Hypersensitivity to tadalafil or any ingredient in the formulation; Stevens-Johnson syndrome and exfoliative dermatitis have been reported.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effect of tadalafil is headache.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The manufacturer states that safety and efficacy of tadalafil have not been established in pediatric patients with PAH.
Limited published data from a randomized controlled trial, observational studies, and case series of tadalafil use in pregnant females have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Pregnant women with untreated PAH are at risk for heart failure, stroke, preterm delivery, and maternal and fetal death. Experts recommend that patients with PAH avoid pregnancy.
Tadalafil and/or its metabolites cross the placenta, resulting in fetal exposure in rats. In animal reproduction studies, no adverse developmental effects were observed with oral administration of tadalafil to pregnant rats or mice during organogenesis at exposures up to 7 times the maximum recommended human dose (MRHD) of 40 mg/day based on AUC.
There are no data on the presence of tadalafil and/or its metabolites in human milk, the effects on the breastfed child, or the effects on milk production.
Tadalafil and/or its metabolites are present in the milk of lactating rats at concentrations approximately 2.4-times that found in the plasma. The manufacturer states when a drug is present in animal milk, it is likely that the drug will be present in human milk.
The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for tadalafil and any potential adverse effects on the breastfed child from the drug or from the underlying maternal condition.
Tadalafil dosage adjustment based solely on age is not necessary in geriatric patients.
Safety of tadalafil in geriatric patients (>65 and >=75 years of age) is similar to that in younger patients. The manufacturers state that modification of tadalafil dosage is not needed in geriatric patients solely on the basis of age; however, the possibility of greater sensitivity in some geriatric individuals should be considered.
Compared to healthy subjects 19-45 years of age, clearance was lower, AUC increased 25%, and no effect on peak plasma concentration was observed in elderly (>=65 years of age) males given a 10 mg dose of tadalafil.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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