Vardenafil

Registered South African indications:

• Erectile dysfunction

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Coadministration with nitrates or nitric oxide donors
• Vardenafil is contraindicated in patients who have loss of vision in one eye because of non-arteritic anterior ischaemic optic neuropathy (NAION), regardless of whether this episode was in connection or not with previous phosphodiesterase 5 (PDE5) inhibitor exposure
• Women, new-borns and children
• End-stage renal disease requiring dialysis
• Anatomical deformation of the penis (such as angulation, cavernosal fibrosis or Peyronie’s disease)
• Conditions which may predispose to priapism (such as sickle cell anaemia, multiple myeloma or leukaemia)
• Hypotension (resting systolic blood pressure of < 90 mmHg)
• Uncontrolled hypertension (> 170/110 mmHg)
• Recent history of stroke, life-threatening arrhythmia or myocardial infarction (within last 6 months)
• Uncontrolled cardiac failure
• Unstable angina
• Known hereditary degenerative retinal disorders such as retinitis pigmentosa
• Bleeding disorders
• Active peptic ulceration
• Severe impairment of liver function
• Concomitant use of vardenafil with the HIV protease inhibitors indinavir and ritonavir
• Moderate hepatic impairment (10mg odt)
• People with phenylketonuria (10mg odt)
• Patients with rare hereditary fructose intolerance (10mg odt)

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment (CrCl ≥15-<30ml/min)
• Mild to moderate hepatic impairment (fct)
• Mild hepatic impairment (odt)
• Elderly
• Cardiovascular disease
• Left ventricular outflow obstruction
• Anatomical deformities of the penis
• Conditions predisposing to priapism
• Risk factors for QT prolongation
• Bleeding disorders
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: tab

Erectile dysfunction

• Oral (tab): Initial: 10mg, 1hr before sexual activity; Dosing range: 5-20mg, dly; Max frequency: 1 dose/day; Max: 20mg/24hrs

Medicine may be taken anywhere from 25 minutes to at least up to 4 to 5 hours before sexual activity

Sexual stimulation is required for a natural response to treatment

Not established for use in children

Pregnancy

• Caution; not recommended
• Not indicated for use in women
• There are no studies of vardenafil in pregnant women

Breastfeeding

• Caution; not recommended
• Not indicated for use in women

Fertility

• There are no fertility data available

Renal Impairment

• CrCl ≥30ml/min: No dose adjustment recommended
• CrCl ≥15-<30ml/min: Caution; dose adjustment recommended
  Consider an initial dose of 5mg; Based on tolerability and efficacy the dose may subsequently be increased to 10-20mg
• End-stage renal disease requiring dialysis: Contraindicated

Hepatic Impairment

• Mild (Child-Pugh class A): Caution; no dose adjustment recommended
• Moderate (Child-Pugh class B): Caution; dose adjustment recommended
  Consider an initial dose of 5mg, which may subsequently be increased to 10mg
• Moderate (Child-Pugh class B): Contraindicated (10mg odt)
• Severe (Child-Pugh class C): Contraindicated

Elderly

• Caution; no dose adjustment recommended
  Consider an initial dose of 5mg
  Increase in dose should be carefully considered depending on individual tolerability; Max: 20mg/24hrs 

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Dizziness
• Somnolence
• Paraesthesia
• Dysaesthesia
• Syncope 
• Seizure
• Amnesia
• Sleep disorder
• Anxiety

Cardiovascular Disorders

• Palpitations
• Tachycardia
• Myocardial infarction
• Ventricular tachyarrythmias
• Angina pectoris
• Flushing
• Hypotension
• Hypertension
• Chest pain

Respiratory Disorders

• Nasal congestion
• Dyspnoea
• Sinus congestion
• Epistaxis

Gastrointestinal Disorders

• Dyspepsia
• Gastro-oesophageal reflux disease
• Gastritis
• Abdominal pain
• Diarrhoea
• Nausea and vomiting
• Dry mouth

Hepatobiliary Disorders

• Increased transaminases
• Increased gamma glutamyltransferase

Genitourinary Disorders

• Haematuria
• Increase in erection
• Priapism
• Penile haemorrhage
• Haematospermia

Musculoskeletal Disorders

• Back pain
• Increase in creatine phosphokinase
• Myalgia
• Increased muscle tone and cramping

Skin and Subcutaneous Tissue Disorders

• Erythema
• Rash
• Photosensitivity reaction

Immune, Blood and Lymphatic System Disorders

• Allergic oedema 
• Angioedema
• Allergic reaction

Sensory Disorders

• Conjunctivitis
• Visual disturbances
• Ocular hyperaemia
• Visual colour distortions
• Eye pain 
• Photophobia
• Increased intraocular pressure
• Increased lacrimation 
• Non-arteritic anterior ischaemic optic neuropathy
• Visual defects
• Tinnitus
• Vertigo
• Sudden deafness

• Alpha blockers 
• CYP3A4 inhibitors
• Ketoconazole
• Itraconazole
• HIV protease inhibitors
• Indinavir
• Ritonavir
• Nicorandil
• Terazosin
• Phosphodiesterase-5 inhibitors 
• Nitrates or nitric oxide donors

None routine

Vardenafil is a selective inhibitor of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDE5), the most abundant phosphodiesterase isoenzyme in the human penile corpus cavernosum. PDE5 is responsible for the degradation of cGMP in the corpus cavernosum. By inhibiting PDE5, vardenafil enhances the effect of endogenous nitric oxide, locally released in corpus cavernosum upon sexual stimulation. The inhibition of PDE5 by vardenafil leads to increased cGMP levels in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 has little effect in the absence of sexual stimulation. Vardenafil thus potentiates the natural response to sexual stimulation.

Tablet 5mg

• Levitra (Bayer) originator

Tablet 10mg

• Levitra (Bayer) originator
• Levitra ODT (Bayer) originator

Tablet 20mg

• Levitra (Bayer) originator