Co-careldopa and Entacapone

Antiparkinsonism Preps · Dopa decarboxylase inhibitor

Indications

Treatment of patients with Parkinson's disease and end-of-dose motor fluctuations not stabilized on levodopa/Dopa-decarboxylase inhibitor treatment.

Dosage

Adults: Only 1 tab to be taken for each dose, as clinically appropriate. Max 10 tabs daily, as per physician's advice. Children: Not recommended.

Adverse Effects

Weight gain or loss, oedema, confusion, insomnia, nightmares, hallucinations, delusions, agitation, anxiety, euphoria, ataxia, numbness, increased hand tremor, muscle twitching, muscle cramps, falling or gait abnormalities, diplopia, blurred vision, dilated pupils, dry mouth, bitter taste, dysphagia, hiccups, abdominal pain, constipation, diarrhoea, flatulence, flushing, increased sweating, dark sweat, rash, hair loss, urinary retention, urinary incontinence, weakness, faintness, fatigue, headache, malaise, bizarre breathing patterns, neuroleptic malignant syndrome.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Severe hepatic impairment, narrow-angle glaucoma, pheochromocytoma. Concomitant use of MAO inhibitors. History of neuroleptic malignant syndrome and/or non-traumatic rhabdomyolysis. Drug-induced extrapyramidal reactions. Precautions: Use with caution in patients with severe cardiovascular or pulmonary disease, bronchial asthma, renal, hepatic or endocrine disease, or history of peptic ulcer disease or convulsions. Monitor cardiac function in patients with a history of myocardial infarction who have residual atrial nodal or ventricular arrhythmias. Monitor carefully for the development of mental changes, depression or suicidal tendencies while on therapy. Use with caution in patients with chronic wide-angle glaucoma. This product can induce orthostatic hypotension.

Interactions

MAO inhibitors, antipsychotics, dopamine receptor antagonists, anti-hypertensives, antidepressants, phenytoin, CYP2C9 substrates.

Advice to Patient

Take atleast 30 minutes before meals. To reduce GI upset, take with meals. Take at the same time each day. Do not crush sustained release form. Contact prescriber if there is unrelieved constipation, diarrhoea, vomiting, acute headache, dizziness, chest pain, irregular heartbeat, nervousness, loss of memory, hallucinations, seizures, painful or difficult urination, skin rash, increased sedation or dizziness, increased muscle spasm, rigidity or involuntary movements, abdominal pain, blood in stool or if there is worsening of condition. Do not take OTC sedatives and CNS depressants without consulting prescriber. Avoid alcohol during therapy. Take sufficient amount of fluids (2-3 litres per day) to maintain hydration, unless restricted by the prescriber. Change position slowly from sitting or lying to standing. For nasal congestion or dry skin, consult prescriber for relief. Avoid…

Pharmacokinetics

CO-CARELDOPA: Absorption: Absorption of levodopa may be decreased with high-fat, high-calorie or high-protein meal. Metabolism: Levodopa has 2 major pathways (decarboxylation and O-methylation) and 2 minor pathways (transamination and oxidation) of metabolism; Carbidopa inhibits the decarboxylation of levodopa to dopamine in the peripheral tissue to allow greater levodopa distribution into the CNS. Bioavailability: Controlled and extended release: Levodopa: Bioavailability is approx. 70%-75% relative to availability from immediate release formulation; Carbidopa: Bioavailability is approx. 50%-58% relative to availability from immediate release formulation. Intestinal gel: Levodopa: Similar bioavailability relative to oral administration of tablet formulations (81%-98%). Intestinal suspension: Levodopa: 97% relative to oral immediate release tablets. Half-life elimination: Immediate…

Unlicensed Use

Children: Dopamine-sensitive dystonias including Segawa syndrome and dystonias related to cerebral palsy: Expressed as levodopa. 3 mth-18 yr, initially 250 mcg/kg 2-3 times daily of a preparation containing 1:4 carbidopa:levodopa, increased according to response every 2-3 days to max 1 mg/kg three times daily. Treatment of defects in tetrahydrobiopterin synthesis and dihydrobiopterin reductase deficiency: Expressed as levodopa. Neonate, initially 250-500 mcg/kg 4 times daily of a preparation containing 1:4 carbidopa:levodopa, increased according to response every 4-5 days to maintenance dose of 2.5-3 mg/kg 4 times daily; at higher doses consider preparation containing 1:10 carbidopa:levodopa; review regularly, every 3-6 mth; 1 mth-18 yr, initially 250-500 mcg/kg 4 times daily of a preparation containing 1:4 carbidopa:levodopa, increased according to response every 4-5 days to…

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.