Tadalafil is a medication primarily used to treat erectile dysfunction (ED) and symptoms of benign prostatic hyperplasia (BPH), a condition where the prostate gland becomes enlarged. It belongs to a class of drugs called phosphodiesterase type 5 (PDE5) inhibitors.

Tadalafil works by increasing blood flow to the penis during sexual stimulation, which helps men achieve and maintain an erection. It does this by inhibiting the action of PDE5, an enzyme that breaks down cyclic guanosine monophosphate (cGMP), a substance that relaxes smooth muscles and increases blood flow in the penis.

Cialis and adcirca are two brand names for the medication tadalafil. Tadalafil is a phosphodiesterase inhibitor that relaxes the smooth muscles. It causes an erection by increasing blood flow to the penis. It also improves blood flow to the lungs, lowering pulmonary vascular pressures.

Other phosphodiesterase inhibitors include Vardenafil (Levitra) and sildenafil (Viagra)

It is used to treat the following conditions:

• Erectile dysfunction (Cialis only):
  • In order to treat erectile dysfunction, it is utilized.
• Benign prostatic hyperplasia (Cialis only):
  • It is used to address the clinical symptoms of benign prostatic hyperplasia (BPH).
• ED and benign prostatic hyperplasia (Cialis only):
  • ED and the symptoms of BPH are both treated with it.
• Off Label Use of Tadalafil in Adults:
  • Raynaud phenomenon uses it
• Pulmonary arterial hypertension (Adcirca only):
  • It is used to increase exercise capacity in the treatment of pulmonary arterial hypertension (World Health Organization group 1).

Tadalafil (Cialis, adcirca) Dose in Adult

Tadalafil dosage for benign prostatic hyperplasia:

• The typical dose of tadalafil, the active ingredient in Cialis, is 5 milligrams taken orally once a day.

Note: If you're starting BPH treatment with both tadalafil and finasteride, it's usually recommended to continue for no more than 26 weeks.

When you're taking tadalafil alongside certain other medications, adjustments may be needed:

• Alpha-blockers: It's generally not advised to combine tadalafil with alpha-blockers for BPH treatment.
• Strong CYP3A4 inhibitors: In cases where you're using strong CYP3A4 inhibitors alongside tadalafil, the dose is reduced to 2.5 milligrams once daily, with the maximum dose being 2.5 milligrams once daily.

Tadalafil Dose in the treatment of Erectile dysfunction (Cialis):

• As-needed dosing:
  • Take 10 milligrams at least 30 minutes before expected sexual activity, as a single dose.
  • Don't take more than one dose per day.
  • Your doctor may adjust the dose based on how well you tolerate it, within a range of 5 to 20 milligrams.
  • It's worth noting that the effects of a single dose can last for up to 36 hours.
• Once-daily dosing:
  • Take 2.5 milligrams once a day around the same time each day, regardless of when sexual activity is anticipated.
  • Your doctor may adjust this dose based on your tolerability, ranging from 2.5 to 5 milligrams per day.

When taking tadalafil with other medications:

• Alpha-blockers: You should already be stable on alpha-blocker therapy before starting tadalafil, and when you do start, it's typically at the lowest recommended dose.
• Strong CYP3A4 inhibitors: If you're using these alongside tadalafil:
  • For as-needed dosing, the maximum dose is 10 milligrams, but not more often than once every 72 hours.
  • For once-daily dosing, the maximum is 2.5 milligrams once daily.

Tadalafil Dose in the therapy of Pulmonary arterial hypertension (Adcirca):

• For treating pulmonary arterial hypertension (PAH) with Adcirca (tadalafil), the typical dose is 40 milligrams taken orally once a day.

When using tadalafil alongside ritonavir:

• If you're starting tadalafil while already taking ritonavir for at least a week, begin with 20 milligrams once daily. You can increase this to 40 milligrams once daily depending on how well you tolerate it.
• If you're starting ritonavir while already taking tadalafil, stop taking tadalafil at least 24 hours before starting ritonavir. After being on ritonavir for at least a week, resume tadalafil at 20 milligrams once daily, and then, if needed, increase to 40 milligrams once daily based on your tolerability.

Tadalafil Dose in the therapy of Raynaud phenomenon (off-label):  

• The typical dose is 20 milligrams taken orally every other day.
• Clinical trials have lasted from 4 to 8 weeks, either as a standalone treatment or alongside other vasodilator therapies such as calcium channel blockers, ACE inhibitors, or ARBs.

Tadalafil (Cialis, adcirca) Dose in Children

Not advised for use with children

Pregnancy Risk Factor B

• Tadalafil has a Pregnancy Risk Factor B, meaning it might cross the placenta, according to studies.
• It's particularly important for women with pulmonary arterial hypertension to avoid pregnancy, as advised by medical experts.
• Interestingly, in healthy males, very small amounts (less than 0.0005%) of tadalafil are found in semen.

Tadalafil use during breastfeeding:

• The presence of tadalafil in breast milk is not yet known for certain.
• Therefore, caution is advised when considering its use in breastfeeding women, according to the manufacturer's recommendation.

Tadalafil (Cialis, adcirca) Dose in Kidney Disease:

Benign Prostatic Hyperplasia (BPH) (Cialis):

• Creatinine Clearance (CrCl) ≥51 mL/minute: No dosage adjustment needed.
• CrCl 30 to 50 mL/minute: Start with 2.5 mg once daily; maximum dose is 5 mg once daily.
• CrCl <30 mL/minute: Not recommended for use.
• End-Stage Renal Disease (ESRD) requiring hemodialysis: Not recommended for use.

Erectile Dysfunction (Cialis):

• As-needed use:
  • CrCl ≥51 mL/minute: No dosage adjustment necessary.
  • CrCl 30 to 50 mL/minute: Start with 5 mg once daily; maximum dose is 10 mg (not more frequently than every 48 hours).
  • CrCl <30 mL/minute: Maximum dose is 5 mg (not more frequently than every 72 hours).
  • ESRD requiring hemodialysis: Maximum dose is 5 mg (not more frequently than every 72 hours).
• Once-daily use:
  • CrCl ≥31 mL/minute: No dosage adjustment necessary.
  • CrCl <30 mL/minute: Not recommended for use.
  • ESRD requiring hemodialysis: Not recommended for use.

Pulmonary Arterial Hypertension (Adcirca):

• CrCl 31 to 80 mL/minute: Start with 20 mg once daily; increase to 40 mg once daily based on individual tolerability.
• CrCl ≤30 mL/minute: Avoid use due to increased tadalafil exposure, limited clinical experience, and lack of ability to influence clearance by dialysis.
• ESRD requiring hemodialysis: Avoid use due to increased tadalafil exposure, limited clinical experience, and lack of ability to influence clearance by dialysis.

Tadalafil (Cialis, adcirca) Dose in Liver Disease:

Benign Prostatic Hyperplasia (BPH) (Cialis):

• Mild to moderate hepatic impairment (Child-Pugh class A or B): Use cautiously; once-daily use not extensively studied.
• Severe hepatic impairment (Child-Pugh class C): Not recommended for use.

Erectile Dysfunction (Cialis):

• As-needed use:
  • Mild to moderate impairment (Child-Pugh class A or B): Use cautiously; dose should not exceed 10 mg once daily. Once-daily use not extensively evaluated.
  • Severe impairment (Child-Pugh class C): Not recommended for use.
• Once-daily use:
  • Mild to moderate impairment (Child-Pugh class A or B): Use cautiously; once-daily use not extensively evaluated.
  • Severe impairment (Child-Pugh class C): Not recommended for use.

Pulmonary Arterial Hypertension (Adcirca):

• Mild to moderate hepatic impairment (Child-Pugh class A or B): Use cautiously; consider initial dose of 20 mg once daily.
• Severe hepatic impairment (Child-Pugh class C): Avoid use; not studied extensively in severe hepatic cirrhosis patients.

Common Side Effects of Tadalafil (Cialis, adcirca) Include:

• Central Nervous System:
  • Headache
• Cardiovascular:
  • Flushing
• Neuromuscular & Skeletal:
  • Myalgia
  • Limb Pain
• Gastrointestinal:
  • Nausea
• Respiratory:
  • Respiratory Tract Infection
  • Nasopharyngitis

Less Common Side Effects of Tadalafil (Cialis) Include:

• Cardiovascular:
  • Orthostatic Hypotension
  • Palpitations
  • Facial Edema
  • Syncope
  • Tachycardia
  • Hypotension
  • Myocardial Infarction
  • Hypertension
  • Angina Pectoris
  • Chest Pain
  • Peripheral Edema
• Dermatologic:
  • Pruritus
  • Diaphoresis
  • Skin Rash
• Central Nervous System:
  • Fatigue
  • Pain
  • Hypoesthesia
  • Insomnia
  • Dizziness
  • Drowsiness
  • Paresthesia
  • Vertigo
• Endocrine & Metabolic:
  • Increased Gamma-Glutamyl Transferase
• Genitourinary:
  • Urinary Tract Infection
  • Spontaneous Erections
  • Prolonged Erection
• Gastrointestinal:
  • Vomiting
  • Xerostomia
  • Gastroesophageal Reflux Disease
  • Diarrhea
  • Dyspepsia
  • Gastroenteritis
  • Abdominal Pain
  • Gastritis
  • Hemorrhoidal Bleeding
  • Dysphagia
  • Esophagitis
  • Loose Stools
  • Upper Abdominal Pain
• Hepatic:
  • Abnormal Hepatic Function Tests
• Hematologic & Oncologic:
  • Rectal Hemorrhage
• Neuromuscular & Skeletal:
  • Asthenia
  • Neck Pain
  • Back Pain
  • Arthralgia
• Otic:
  • Hearing Loss
  • Tinnitus
• Ophthalmic:
  • Increased Lacrimation
  • Vision Color Changes
  • Conjunctivitis
  • Eyelid Edema
  • Blurred Vision
  • Conjunctival Hyperemia
  • Eye Pain
• Renal:
  • Renal Insufficiency
• Respiratory:
  • Epistaxis
  • Pharyngitis
  • Upper Respiratory Tract Infection
  • Cough
  • Nasal Congestion
  • Paranasal Sinus Congestion
  • Dyspnea

Contraindication to (Cialis, Adcirca) Tadalafil Include:

• Tadalafil should not be used if you have a serious allergy to tadalafil itself or any part of the medicine.
• Also, if you're taking organic nitrates regularly or sometimes, or medications that stimulate guanylate cyclase like riociguat, using tadalafil is not safe.
• In Canada, there's an extra caution: if you've had a previous episode of nonarteritic anterior ischemic optic neuropathy, tadalafil isn't recommended.

Warnings and precautions

Angina chest pain

• If you have anginal chest pain after taking tadalafil, it's crucial to seek immediate medical help.

Color discrimination:

• Tadalafil may affect color vision, especially at higher doses.
• If you have retinitis pigmentosa or other genetic retinal disorders, there isn't enough safety information available.
• So, use caution when taking tadalafil.

Hearing loss:

• Rarely, tadalafil has been associated with sudden hearing loss or a decrease in hearing.
• This might come with symptoms like ringing in the ears (tinnitus) and dizziness.
• If you experience a sudden decrease in hearing or loss of hearing while taking tadalafil, it's important to seek medical help promptly.
• While there isn't a confirmed direct link between tadalafil use and hearing loss, it's crucial to address any changes in hearing promptly.

Priapism

• Tadalafil use has been associated, though rarely, with priapism, which is a prolonged and painful erection lasting more than 6 hours.
• If you experience an erection lasting more than 4 hours, it's crucial to seek medical help promptly.
• Patients with conditions like sickle cell anemia, multiple myeloma, or leukemia should use tadalafil with caution, as they might be more prone to priapism.

Hypotension

• Tadalafil can cause decreases in blood pressure because of its ability to widen blood vessels.
• This effect may be a concern for individuals with left ventricular outflow obstruction, such as aortic stenosis or hypertrophic obstructive cardiomyopathy, who might be more sensitive to low blood pressure.
• When tadalafil is used alongside alpha-adrenergic antagonist therapy, it can lead to symptomatic low blood pressure, so patients should start at the lowest possible dose and be hemodynamically stable.
• Additionally, it's advised to avoid or limit substantial alcohol consumption, as it can increase the risk of symptomatic low blood pressure.

Vision loss:

• Vision loss, though rare, could indicate a condition called nonarteritic anterior ischemic optic neuropathy (NAION), but it's not certain if there's a direct link to PDE5 inhibitors like tadalafil.
• If you suddenly lose vision in one or both eyes while taking tadalafil, stop using it and seek medical help right away.
• People who've had NAION before are at higher risk of it happening again.
• Factors like having a "crowded disc" in the eye, coronary artery disease, diabetes, high blood pressure, high cholesterol, smoking, and being over 50 also increase the risk.
• Tadalafil should be used cautiously in these cases, only if the benefits outweigh the risks.
• It's not recommended for use in people with known hereditary degenerative retinal disorders like retinitis pigmentosa, as its safety hasn't been evaluated in these patients.

Anatomical penis deformation:

• Tadalafil should be used cautiously in individuals with anatomical deformities of the penis, such as angulation, cavernosal fibrosis, or Peyronie's disease.

Bleeding disorders:

• Tadalafil should be used with caution in patients who have bleeding disorders, as its safety and effectiveness haven't been fully established in these cases.
• In laboratory studies, there's been a suggestion that tadalafil might have a reduced effect on platelet aggregation, which could affect blood clotting.

Cardiovascular disease

• Tadalafil isn't recommended for use in patients with certain cardiovascular conditions such as very low blood pressure (hypotension), uncontrolled high blood pressure, recent heart failure, unstable angina, recent stroke or heart attack, or certain arrhythmias.
• Safety and effectiveness haven't been evaluated in these cases.
• For pulmonary arterial hypertension (PAH), it's not evaluated in patients with significant valve disease, severe arrhythmias, low blood pressure, uncontrolled high blood pressure, severe left heart dysfunction, certain heart muscle disorders, or significant coronary artery disease.
• Caution is advised in patients with left ventricular outflow obstruction, like aortic stenosis or hypertrophic obstructive cardiomyopathy, as they may be more sensitive to the blood vessel-widening effects of tadalafil.
• Since sexual activity carries some cardiac risk, doctors may consider assessing their patients' cardiovascular health before starting any erectile dysfunction treatment.

Hepatic impairment

• Tadalafil should be used cautiously in patients with mild to moderate hepatic impairment, as dosage adjustments or limitations might be necessary.
• However, it's not recommended for use in patients with severe hepatic impairment or cirrhosis.

Peptic ulcer disease:

• Tadalafil should be used cautiously in patients with active peptic ulcer disease due to its potential effect on platelets, which could increase the risk of bleeding.
• However, its safety and effectiveness haven't been fully established in these cases.

Pulmonary Venoocclusive Disease (PVOD),

• For individuals with pulmonary veno-occlusive disease (PVOD), the use of pulmonary vasodilators like tadalafil isn't recommended.
• There's a concern that these medications might worsen the cardiovascular condition in PVOD patients.
• Additionally, there's no clinical data available regarding the use of tadalafil in patients with PVOD.
• If a person with unrecognized PVOD develops symptoms of pulmonary edema while taking tadalafil, it's important to investigate the possibility of PVOD.

Renal impairment

• Tadalafil should be used cautiously in patients with renal impairment, and dosage adjustment or limitation might be necessary.

Monitor:

Blood Pressure, Response, and Adverse Effects:

• Tadalafil can affect blood pressure, potentially leading to low blood pressure (hypotension).
• Some people might experience side effects such as dizziness or fainting due to changes in blood pressure.
• It's essential to monitor blood pressure regularly, especially when starting or adjusting tadalafil treatment.

Urine Flow and PSA (Prostate-Specific Antigen):

• Tadalafil can help improve urine flow in conditions like benign prostatic hyperplasia (BPH).
• It's important to keep an eye on PSA levels, as tadalafil might affect them. PSA levels are sometimes used to monitor prostate health and screen for prostate cancer.

How to administer Tadalafil (Cialis, adcirca)?

Oral Administration:

• Tadalafil can be taken with or without food, according to personal preference or as advised by a healthcare provider.

Adcirca:

• The daily dose of Adcirca should be taken all at once; it's not recommended to split the dose throughout the day.

Cialis:

• Tablets of Cialis should not be split; the entire dose should be taken as prescribed.
• When used on an as-needed basis for erectile dysfunction, take Cialis at least 30 minutes before sexual activity.
• When used on a once-daily basis, take Cialis at the same time each day, regardless of sexual activity timing.

Mechanism of action of Cialis (Tadalafil):

Benign Prostatic Hyperplasia (BPH):

• The exact mechanism of tadalafil's effects on BPH is not fully understood.
• It's believed that tadalafil works by reducing smooth muscle and endothelial cell growth, decreasing nerve activity, and increasing relaxation of smooth muscles in the prostate and bladder.

Erectile Dysfunction (ED):

• Tadalafil doesn't directly cause penile erections but enhances the body's response to sexual stimulation.
• During sexual arousal, nitric oxide (NO) is released in the penis, leading to increased levels of cyclic guanosine monophosphate (cGMP), which relaxes smooth muscles and increases blood flow to the penis.
• Tadalafil inhibits phosphodiesterase type 5 (PDE-5), an enzyme responsible for breaking down cGMP, leading to increased levels of cGMP in the penis.
• With sexual stimulation, tadalafil helps maintain higher levels of cGMP, promoting smooth muscle relaxation and improved blood flow to the penis, aiding in achieving and maintaining an erection.

Pulmonary Arterial Hypertension (PAH):

• Tadalafil inhibits phosphodiesterase type 5 (PDE-5) in the smooth muscle of the pulmonary vasculature.
• PDE-5 is responsible for breaking down cyclic guanosine monophosphate (cGMP).
• By inhibiting PDE-5, tadalafil increases the concentration of cGMP, leading to relaxation of the pulmonary blood vessels.
• This relaxation results in vasodilation, primarily in the pulmonary circulation and to a lesser extent in the systemic circulation, helping to reduce pulmonary arterial pressure.

Onset of Action:

• Tadalafil typically starts working within 1 hour after administration.

Peak Effect (Pulmonary Artery Vasodilation):

• The peak effect of pulmonary artery vasodilation occurs approximately 75 to 90 minutes after taking tadalafil.

Duration:

• For erectile dysfunction, the effects of tadalafil can last for up to 36 hours.

Distribution:

• Tadalafil has a distribution volume of 63 to 77 liters.

Protein Binding:

• Approximately 94% of tadalafil in the bloodstream is bound to proteins.

Metabolism:

• Tadalafil is primarily metabolized in the liver by the enzyme CYP3A4 into inactive metabolites.

Half-Life Elimination:

• The elimination half-life of tadalafil is 15 to 17.5 hours.
• In patients with pulmonary hypertension who are not receiving bosentan, the half-life is extended to 35 hours.

Time to Peak, Plasma:

• Tadalafil reaches peak plasma levels around 2 hours after administration, with a range of 30 minutes to 6 hours.

Excretion:

• Tadalafil is primarily excreted through feces (approximately 61%, mostly as metabolites) and urine (approximately 36%, also mostly as metabolites).

International Brands of Tadalafil:

• ACT Tadalafil
• Adcirca
• Auro-Tadalafil
• Cialis
• JAMPTadalafil
• RAN-Tadalafil
• 36 Horas
• Adafil
• Adcirca
• Cendom
• Cendom Orally Soluble Film
• Cialis
• Ciaton
• Digram
• Duralis
• Erectalis
• Mar-Tadalafil
• MINT-Tadalafil
• Erotadil
• Exerdya
• Forzest
• Glodafil
• APO-Tadalafil
• APO-Tadalafil PAH
• Glofil
• GODN Orodispersible Film
• Greseo Powd.
• Gugu Chew
• Jovan T 20
• Lanrextan
• Link
• Mega Joy
• Megafil
• Megafort
• RIVATadalafil
• TEVA-Tadalafil
• Mplify
• Pasport
• Snafi
• Spciafil
• Sunka
• Tadacip
• Tadaf
• Tadair
• MYLAN-Tadalafil
• Priva-Tadalafil
• Cialis
• Adcirca
• Alyq
• Tadam
• Taderect
• Tagra
• Talmanco
• Tyra
• Viev
• Yesgra
• Zenavil
• Zydalis

Tadalafil (Cialis, adcirca) Brands in Pakistan:

No Brands Available in Pakistan.