Saquinavir

Registered South African indications:

• HIV-1 infection

Contraindications

• Hypersensitivity to the active ingredient or to any of its excipients
• Coadministration with astemizole and cisapride
• Coadministration with certain medicines, as detailed below, which may result in potentially life-threatening side effects:
  • Antiarrhythmics: Amiodarone, flecainide, propafenone – Life-threatening cardiac dysrhythmia
  • Antihistamines: Astemizole, terfenadine – Life-threatening cardiac dysrhythmia
  • Ergot derivatives: Dihydroergotamine, ergonovine, ergotamine, methylergonovine – Acute ergot toxicity
  • GI motility Agent: Cisapride – Life-threatening cardiac dysrhythmia
  • HMG-CoA reductase inhibitors: Simvastatin, lovastatin – Rhabdomyolysis
  • Neuroleptic: Pimozide – Life-threatening cardiac dysrhythmia
  • Sedatives/hypnotics: Triazolam, midazolam – Prolonged/increased sedation
  • Antimycobacterial agent: Rifampicin – Severe hepatocellular toxicity
  • Others: Garlic, St John’s wort – Decreased plasma concentrations
• Ritonavir-boosted saquinavir is contraindicated in patients with congenital or documented acquired QT prolongation and electrolyte disturbances, particularly uncorrected hypokalaemia or hyperkalaemia
• Coadministration of ritonavir-boosted saquinavir with medicines that have both pharmacokinetic interactions and prolong QT and/or PR intervals
• Pregnancy
• Lactation
• Children under 16 years of age
• Limited experience is available in patients older than 60 years
• Severe hepatic impairment

Cautions

• Severe renal impairment
• Moderate hepatic impairment
• Elderly
• Use without ritonavir boosting
• Women
• High doses
• Chronic diarrhoea
• Malabsorption
• Haemophilia
• Severe immunosuppression
• High body mass index
• Underlying infections
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

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

HIV infection

• Oral (cap): 1000mg, 12hrly, taken with 100mg ritonavir, 12hrly

Not established for use in children below 16 years (see Contraindications)

Consult HIV/infectious disease specialists prior to any decisions related to ARV regimen termination/switch

Pregnancy

• Contraindicated

Breastfeeding

• Contraindicated

Renal Impairment

• Severe: Caution; no dose adjustment recommended

Hepatic Impairment

• Moderate: Caution; no dose adjustment recommended 
• Severe: Contraindicated

Elderly

• Caution; no information available

Central Nervous System Disorders

• Decreased libido 
• Sleep disorder
• Anxiety 
• Irritability 
• Nightmare 
• Suicide attempt
• Paraesthesia 
• Peripheral neuropathy 
• Dizziness 
• Dysgeusia 
• Headache
• Balance disorder
• Cerebellar syndrome
• Disturbance in attention
• Postural dizziness
• Memory impairment
• Movement disorder
• Neuropathic pain
• Circumoral paraesthesia
• Asthenia

Cardiovascular Disorders

• Palpitations
• Hot flush
• Hypotension 
• Vasculitis

Respiratory Disorders

• Dyspnoea
• Asthma
• Nasal ulcer

Gastrointestinal Disorders

• Diarrhoea 
• Nausea and vomiting
• Abdominal distension 
• Abdominal pain
• Constipation
• Dry mouth
• Dyspepsia
• Eructation 
• Flatulence 
• Dry lips
• Loose stools
• Aphthous ulcers
• Aphthous stomatitis 
• Aptyalism
• Dysphagia 
• Epigastric discomfort 
• Gastritis
• Gastro-oesophageal reflux disease 
• Haemorrhoids
• Oral hypoaesthesia
• Mouth ulceration
• Oral discomfort
• Pharyngolaryngeal pain

Genitourinary Disorders

• Haematuria
• Nocturia
• Renal pain
• Urinary frequency
• Breast pain
• Breast hypertrophy

Endocrine and Metabolic Disorders

• Diabetes mellitus
• Anorexia
• Increased appetite
• Hyperglycaemia
• Hyponatraemia
• Increased alanine aminotransferase 
• Increased aspartate aminotransferase 
• Increased cholesterol
• Increased triglycerides 
• Increased low density lipoprotein 
• Decreased platelet count
• Increased amylase 
• Increased bilirubin 
• Increased creatinine 
• Decreased haemoglobin
• Decreased lymphocyte count 
• Decreased white blood cell count
• Elevated pyruvate lactate
• Increased alkaline phosphatase 
• Increased lactate dehydrogenase 
• Increased lactic acid
• Increased gamma-glutamyltransferase
• Abnormal liver function test
• Abnormal partial prothrombin time 
• Raised creatinine phosphate
• Decreased weight
• Increased weight

Musculoskeletal Disorders

• Muscle spasms
• Arthritis
• Muscle cramps
• Upper limb fracture

Skin and Subcutaneous Tissue Disorders

• Lipodystrophy 
• Alopecia 
• Dry skin 
• Eczema 
• Lipoatrophy
• Pruritus
• Rash
• Dandruff 
• Atopic dermatitis
• Heat rash 
• Hyperhidrosis 
• Nail discolouration 
• Pigmentation disorder
• Skin discolouration 
• Skin ulcer
• Spider naevus

Immune, Blood and Lymphatic System Disorders

• Folliculitis
• Oral candidiasis 
• Otitis media
• Perianal abscess
• Pharyngitis
• Stye
• Subcutaneous abscess
• Viral infection
• Anaemia
• Neutropenia
• Hypersensitivity

Sensory Disorders

• Hearing disability
• Abnormal vision

• Antiarrhythmics
• Amiodarone
• Flecainide
• Propafenone
• Antihistamines
• Astemizole
• Terfenadine
• Ergot derivatives
• Dihydroergotamine
• Ergonovine
• Ergotamine
• Methylergonovine
• Gastrointestinal motility agent
• Cisapride
• Sedatives/ hypnotics
• Triazolam
• Midazolam
• Antimycobacterial agent
• Rifampicin
• Alcohol
• Delavirdine
• Atazanavir
• Indinavir
• Lopinavir/ritonavir
• Nelfinavir
• Tipranavir/ritonavir
• Maraviroc
• Cobicistat
• Alfuzosin
• Bepridil
• Warfarin
• Anticonvulsants
• Antidepressants
• Colchicine
• Clarithromycin
• Erythromycin
• Streptogramin antibiotics
• Halofantrine
• Pentamidine
• Sparfloxacin
• Itraconazole
• Fluconazole
• Miconazole
• Rifabutin
• Quetiapine
• Benzodiazepines
• Calcium channel blockers
• Corticosteroids
• Endothelin receptor antagonist
• Digoxin
• HMG-CoA reductase inhibitors
• Simvastatin
• Lovastatin
• Atorvastatin
• Tacrolimus
• Ciclosporin
• Rapamycin
• Salmeterol
• Methadone
• Neuroleptics
• Pimozide
• Oral contraceptives
• Phosphodiesterase type 5 inhibitors
• Proton pump inhibitors
• Ergot alkaloids
• Garlic
• St John's wort
• CYP3A4 substrates
• Diphemanil
• Vincamine

None routine. Specific cases mat require

• ECG
• Hepatic function
• Serum lipids
• Serum electrolytes
• Blood glucose

The HIV protease is an essential viral enzyme required for the specific cleavage of viral gag and gag-pol polyproteins. Saquinavir selectively inhibits the HIV protease, thereby preventing the creation of mature infectious virus particles.

Capsule 200mg

• Invi-Rase (Roche) originator