Drugs used in Parkinsonism & other movement disorders Flashcards
(22 cards)
MOA of levodopa +/- carbidopa
Precursor of dopamine
Carbidopa inhibits peripheral metabolism via dopa decarboxylase
Which types of drugs diminish doses and prolong the actions of levodopa?
COMT inhibitors
MAO B inhibitors
Adverse effects of levodopa
GI upset (emesis)
Dyskinesias in 80% - usually choreoathetosis of the face and distal extremities
Postural hypotension
COMT inhibitors used in the treatment of Parkinson’s disease
Tolcapone
Entacapone (peripheral action only)
MAO-B inhibitors used in the treatment of Parkinson’s disease
Selegiline, rasagiline
*NB serotonin syndrome with meperidine and possibly SSRIs and TCAs
D2 agonists used in the treatment of PD
Bromocriptine (ergot; not frequently used anymore)
Ropinirole - can be used as sole agent in early PD and adjunct to L-dopa. Non-ergot
Apomorphine
D3 agonist used in the treatment of PD
Pramipexole; can be used as sole agent in early PD and adjunct to L-dopa
Injected subcutaneously to provide rapid but temporary relief of “off-periods” of akinesia in patients on optimized dopaminergic therapy
Apomorphine
Common side effects of dopamine agonists
Anorexia, nausea, constipation, postural hypotension, dyskinesias, and mental disturbances (confusion, delusions, and hallucinations)
*NB: mental disturbances occur more frequently with DA receptor activators than with levodopa.
Antimuscarinic agent used in treatment of PD
Benztropine
What symptoms of PD do antimuscarinic agents improve?
Tremor and rigidity but NOT bradykinesia
D2 antagonists used in the treatment of HD
Haloperidol
Perphenazine
Amine-depleting drugs used in the treatment of HD
Reserpine
Tetrabenazine
Side effects of haloperidol
Extrapyramidal dysfunction
Side effects of tetrabenazine
depression, hypotension, sedation
Drugs for Tourette’s syndrome
Haloperidol
Clonidine
- Reduce vocal and motor tic frequency and severity
Drugs for managing essential tremor
Beta blockers: propranolol, metoprolol
What drug is most suitable for management of tremor in a patient who has pulmonary disease?
Metoprolol: it is B1 selective and is equally effective.
D2 agonist that is metabolized by hepatic CYP1A2, and therefore whose plasma levels may be increased by other substrates of this enzyme (including caffeine and warfarin)
Ropinirole
Antiviral used in the treatment of PD
Amantadine
MOA of amantadine
exact mechanism is unknown; increases the neurotransmission of DA, either by increasing synthesis or release of DA or inhibition of DA reuptake
Drugs that can induce parkinsonism
- Butyrophenone and phenothiazine are the most important antipsychotics that cause PD
- Reserpine
- MPTP ( a by-product of the attempted synthesis of an illicit meperidine analog, which causes irreversible parkinsonism through destruction of dopaminergic neurons in the nigrostriatal tract)