Levodopa + Carbidopa + Entacapone Pharmacology

Levodopa + Carbidopa + Entacapone

About Levodopa + Carbidopa + Entacapone
N/A
Mechanism of Action of Levodopa + Carbidopa + Entacapone
Levodopa is the metabolic precurosor of dopamine, it crosses the blood-brain barrier and is converted to dopamine in the brain. Carbidopa increases the amount of levodopa that is transported into the CNS by inhibiting the decarboxylation of peripheral levodopa. Entacapone is a selective inhibitor of catechol-o-methyltransferase. Given concurrently, entacapone results in greater and more substained plasma levels of levodopa, leading to greater control of parkinsonism symptoms
Pharmacokinets of Levodopa + Carbidopa + Entacapone
N/A
Onset of Action for Levodopa + Carbidopa + Entacapone
N/A
Duration of Action for Levodopa + Carbidopa + Entacapone
N/A
Half Life of Levodopa + Carbidopa + Entacapone
N/A
Side Effects of Levodopa + Carbidopa + Entacapone
N/A
Contra-indications of Levodopa + Carbidopa + Entacapone
N/A
Special Precautions while taking Levodopa + Carbidopa + Entacapone
N/A
Pregnancy Related Information
Contraindicated
Old Age Related Information
N/A
Breast Feeding Related Information
Contraindicated
Children Related Information
N/A
Indications for Levodopa + Carbidopa + Entacapone
Parkinson?s Disease
Interactions for Levodopa + Carbidopa + Entacapone
Increased risk of postural hypotension when used concurrently with hypotensive drugs
Dopamine D2 receptor antagonists, phenytoin or papaverine may reduce the efficacy of levodopa
Iron salts may reduce the bioavailability
Typical Dosage for Levodopa + Carbidopa + Entacapone
Optimum dosage must be carefully titrated according to patient's response
Initial: 1 tab/day. Max: 8 tabs/day
Schedule of Levodopa + Carbidopa + Entacapone
N/A
Storage Requirements for Levodopa + Carbidopa + Entacapone
N/A
Effects of Missed Dosage of Levodopa + Carbidopa + Entacapone
N/A
Effects of Overdose of Levodopa + Carbidopa + Entacapone
N/A

Levodopa

About Levodopa
Dopamine agonist, Antiparkinsonian agent.
Mechanism of Action of Levodopa
Levodopa is the precursor of Dopamine.Levodopa crosses the blood brain barrier and undergoes decarboxylation and releases Dopamine. The Dopamine stimulates dopaminergic receptors in the basal ganglia and enhances the balance between cholinergic and dopaminergic activity and results in improved modulation of voluntary nerve impulses transmitted to the motor cortex.
Pharmacokinets of Levodopa
Absorption: It is absorbed rapidly from the small intestine. Distribution: It is widely distributed in most body tissue.It crosses blood brain barrier and also distribute in the milk. Metabolism: About 95% of the drug is converted to Dopamine by l-aromatic amino acid decarboxylase enzyme.Excretion:It is excreted mainly through urine.
Onset of Action for Levodopa
N/A
Duration of Action for Levodopa
5 hour
Half Life of Levodopa
1 - 3 hours
Side Effects of Levodopa
1.Vomiting
2.Nausea
3.Anorexia
4.Aggressive behavior
5.Tardive dyskinesia
6.Ataxia
7.Tremor
8.Nervousness
9.Anxiety
10.Delirium
11.Orthostatic hypotension
12.Bitter taste
13.Hemolytic anemia
14.Agranulocytosis
Contra-indications of Levodopa
1.Hypersensitivity to the drug
2.Concurrent therapy with MAO inhibitors within 14days
3.Acute angle closure glaucoma
4.Melanoma
Special Precautions while taking Levodopa
1.Severe renal impairment
2.Hepatic impairment
3.Pulmonary disorders
4.Myocardial Infarction
5.Arrhythmia
6.Peptic ulcer
7.Osychiatric illness
8.Bronchial asthma
9.Emphysema
10.Endocrine disorders
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Below 12 years:Contraindicated
Indications for Levodopa
1.Parkinsonism
Interactions for Levodopa
N/A
Typical Dosage for Levodopa
Initial dose: 0.5 - 1 g daily in 2 - 4 divided doses with food. Increase 100 - 750mg daily every 3 - 7 days. Maximum dose: 8 g/day
Schedule of Levodopa
H
Storage Requirements for Levodopa
Store at 25 - 30 degree C in a tightly closed container.
Effects of Missed Dosage of Levodopa
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose.
Effects of Overdose of Levodopa
Give supportive measures and symptomatic treatment.Drug can be removed from the body by gastric lavage. To reverse the toxic and therapeutic effect of Levodopa Pyridoxine 10 - 25 mg can be given.

Carbidopa

About Carbidopa
A noncompetitive DOPA decarboxylase inhibitor, Antidyskinetics, Anti-Parkinson`s Agent.
Mechanism of Action of Carbidopa
Carbidopa inhibits the peripheral decarboxylation of Levodopa and thus slowing its conversion to Dopamine in extra cerebral tissues. This results in an increased availability of Levodopa for transport to the brain and undergoes decarboxylation to Dopamine in the brain. Carbidopa increases the concentration of Levodopa in the brain.
Pharmacokinets of Carbidopa
Absorption: About 40 - 70% of the drug is absorbed after oral administration. Distribution: It is widely distributed in body tissues except the CNS. It is also distributed into breast milk. Excretion: It is excreted unchanged in urine.
Onset of Action for Carbidopa
N/A
Duration of Action for Carbidopa
N/A
Half Life of Carbidopa
1 - 2 hours
Side Effects of Carbidopa
1.Vomiting
2.Nausea
3.Anorexia
4.Aggressive behavior
5.Tardive dyskinesia
6.Ataxia
7.Tremor
8.Nervousness
9.Anxiety
10.Delirium
11.Orthostatic hypotension
12.Bitter taste
13.Hemolytic anemia
14.Agranulocytosis
15.Dry mouth
Contra-indications of Carbidopa
1.Hypersensitivity to the drug
2.Concurrent therapy with MAO inhibitors within 14days
3.Acute angle closure glaucoma
4.Melanoma
Special Precautions while taking Carbidopa
1.Severe renal impairment
2.Hepatic impairment
3.Pulmonary disorders
4.Myocardial Infarction
5.Arrhythmia
6.Peptic ulcer
7.Osychiatric illness
8.Bronchial asthma
9.Emphysema
10.Endocrine disorders
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Below 12 years:Contraindicated
Indications for Carbidopa
1.Parkinsonism
Interactions for Carbidopa
N/A
Typical Dosage for Carbidopa
Carbidopa is usually given with Levodopa.Dose is 70 - 100 mg to suppress peripheral decarboxylation of Levodopa.
Schedule of Carbidopa
H
Storage Requirements for Carbidopa
Store at 25 - 30 degree C in a tightly closed container.
Effects of Missed Dosage of Carbidopa
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose.
Effects of Overdose of Carbidopa
Give supportive measures and symptomatic treatment.

Entacapone

About Entacapone
COMT Inhibitor, Systemic Anti-Parkinson`s Agent.
Mechanism of Action of Entacapone
Entacapone is a peripherally acting Catechol O-methyl transferase (COMT) inhibitor. Entacapone block the O- methylation of Levodopa and increases the fraction of the drug available for delivery to the brain. This will result in increased concentration of dopamine and is useful in Parkinsonism.
Pharmacokinets of Entacapone
Absorption: Entacapone is rapidly absorbed after oral administration and the bioavailability is only 35%. Distribution: It is distributed in the body in protein bound form. Metabolism: It is extensively metabolised in the liver. Excretion: It is excreted mainly in faeces and only a small amount in urine.
Onset of Action for Entacapone
10 - 20 minutes
Duration of Action for Entacapone
2 hours
Half Life of Entacapone
3 - 5 hours
Side Effects of Entacapone
1.Nausea
2.Diarrhoea
3.Abdominal pain
4.Urine discoloration
5.Hypotension
6.Drowsiness
7.Hyperkinesia
8.Dyskinesia
9.Dizziness
10.Constipation
11.Dry mouth
12.Dyspepsia
13.Fatigue
14.Confusion
15.Fever
16.Muscle pain
Contra-indications of Entacapone
1.Hypersensitivity to Entacapone
Special Precautions while taking Entacapone
1.Renal impairment
2.Hepatic impairment
3.Patient on monoamine oxidase inhibitor therapy
4.Use caution when driving vehicle, operating machine or involving in any hazardous activities
5.Alcoholics
6.Slowly withdraw the drug with caution
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Contraindicated.
NEONATES: contraindicated
Indications for Entacapone
1. Adjunct to Levodopa or Carbidopa for the treatment of idiopathic Parkinson`s disease
Interactions for Entacapone
No interaction of entacapone with carbidopa has been observed with the recommended treatment schedule. The experience of the clinical use of entacapone with several drugs, including MAO-A inhibitors, tricyclic antidepressants, noradrenaline reuptake inhibitors such as desipramine, maprotiline and venlafaxine, and medicinal products that are metabolised by COMT is limited.
Typical Dosage for Entacapone
Adult: 200 mg with Carbidopa or Levodopa
Maximum daily dose: 1600 mg / day
Schedule of Entacapone
N/A
Storage Requirements for Entacapone
Store at 15 - 30 degree C. Protect from moisture and heat. Keep out of the reach of children.
Effects of Missed Dosage of Entacapone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Entacapone
Give supportive measures and symptomatic treatment. Gastric lavage can be done to increase the elimination of the drug. Activated charcoal is given to reduce the absorption of the drug.

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