Iloprost

Intravenous
Peripheral vascular disease
Adult: Severe chronic lower limb ischaemia in patients at risk of amputation, in whom surgical revascularisation or angioplasty has failed; Severe Raynaud's phenomenon in patients with progressive trophic disorders: Initially, 0.5 ng/kg/minute, if tolerated, may increase in steps of 0.5 ng/kg/minute every 30 minutes up to max dose of 2.0 ng/kg/minute, given over 6 hours daily via IV infusion. Treatment duration: Severe chronic lower limb ischaemia: given for up to 4 weeks; Severe Raynaud's phenomenon: given for 5 consecutive days, repeat cycles at intervals of at least 4 weeks (preferably 6-12 weeks).
Renal impairment: Renal insufficiency requiring dialysis: Reduce dose.
Hepatic impairment: Severe: Reduce dose.
Reconstitution: IV: For use in an infusion pump: reconstitute ampoules labelled as 100 mcg and 50 mcg with 500 mL and 250 mL of diluent respectively. For use with an infusion syringe pump: reconstitute ampoules labelled as 100 mcg and 50 mcg with 50 mL and 25 mL of diluent respectively.

Inhalation
Pulmonary hypertension
Adult: In patients with NYHA functional class III, to improve exercise capacity and symptoms: Initially, 2.5 mcg per dose, if tolerated, may increase to 5 mcg per dose. Administer doses 6-9 times daily according to individual need and tolerability.
Hepatic impairment: Mild to severe: Increase dose interval to 3-4 hourly.

Pulmonary oedema, pulmonary hypertension due to venous occlusive disease, congenital or acquired valvular defects with clinically relevant myocardial function disorders not related to pulmonary hypertension, systolic blood pressure below 85 mmHg, acute or chronic CHF (NYHA II-IV), severe coronary heart disease or unstable angina, MI within the last 6 months, decompensated cardiac failure (unless under close medical supervision), severe arrhythmias, cerebrovascular events (e.g. TIA, stroke) within the last 3 months, active peptic ulcers, trauma, intracranial haemorrhage. IV: Pregnancy and lactation.

Patient with active COPD, severe asthma, acute pulmonary infections. Avoid abrupt withdrawal. Renal and hepatic impairment. Inhalation: Pregnancy and lactation. Patient Counselling This medicine may cause dizziness, if affected, do not drive or operate machinery. Avoid contact to mucous membranes. Monitoring Parameters Monitor heart rate, blood pressure, respiratory rate and for improvements of pulmonary function.

Significant: Syncope. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal discomfort, abdominal pain. General disorders and administration site conditions: Pain, pyrexia, chills, infusion site reactions (e.g. pain, erythema, phlebitis). Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Jaw pain, myalgia, arthralgia, trismus. Nervous system disorders: Dizziness, headache, palpitations, restlessness, drowsiness. Psychiatric disorders: Confusional state. Respiratory, thoracic and mediastinal disorders: Cough, throat irritation. Skin and subcutaneous tissue disorders: Rash, hyperhidrosis. Vascular disorders: Flushing, vasodilation.
Potentially Fatal: Cerebrovascular stroke, myocardial infarction, pulmonary embolism, cardiac failure, convulsion, hypotension, tachycardia, asthma, angina pectoris, dyspnoea, pulmonary oedema, cerebral and intracranial haemorrhage.

Additive hypotensive effect with other vasodilators and antihypertensive agents. Increased risk of bleeding with anticoagulants and platelet aggregation inhibitors.

Iloprost, a synthetic prostacyclin analogue, is a vasodilating agent. It dilates systemic and pulmonary vascular beds, alters pulmonary vascular resistance, and suppresses vascular smooth muscle proliferation. In addition, it is also a mild endogenous inhibitor of platelet aggregation when aerosolised.
Duration: 30-60 minutes (inhalation).
Absorption: Time to peak plasma concentration: Within 5 minutes (inhalation).
Distribution: Volume of distribution: 0.7-0.8 L/kg. Plasma protein binding: Approx 60%, mainly to albumin (IV).
Metabolism: Metabolised in the liver via β-oxidation of the carboxyl side chain.
Excretion: Mainly via the urine (68% as metabolites); faeces (12%). Elimination half-life: 20-30 minutes.

Inhalation: Solution for nebulisation: Store between 20-25°C. Intravenous: Solution for infusion: Store below 30°C.

Other Cardiovascular Drugs

B01AC11 - iloprost ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.