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Pharmacology
Parkinsons Qs
| Question | Answer |
|---|---|
| 1. What neurons are lost in PD? | Dompaminergic neurons |
| 2. How is Parkinson’s disease Tx? | By enhancing dopaminergic activity |
| 3. Why is Dopamine not used in Tx? | Dopamine doesn’t cross BBB |
| 4. In biosynthesis of dopamine what is the rate limiting step? | Tyroxine hydroxylase |
| 5. How is dopaminergic content measured? | Measure Tyroxine hydroxylase |
| 6. What converts Dopa(L-dopa) to Dopamine? | DOPA decarboxylase |
| 7. How are Norepinephrine and Epinephrine (Noreadrenaline n’ adrenaline) related to Dopamine? | They are derivatives of Dopamine |
| 8. What percentage of L dopa reach the dopaminergic neurons? | Very little 1-5% |
| 9. What happens to the remaining L-dopa? | Metabolized elsewhere, periphery |
| 10. What is the problem of having L-dopa metabolized elsewhere? | Causes wide variety of ADR |
| 11. What Rx work at the Dopaminergic nerve terminal? | Levodopa, Selegilline, Amantadine, Ropinirole, Pramipexole, Bromocriptine, Apomorphine, Lisuride, Pergolide |
| 12. What type of neurons are required by L-dopa? | Nigrostriatal neurons |
| 13. What results in the feedback inhibition of L-dopa? | Reduction in endogenous formation of L-dopa |
| 14. What happens to the L-dopa response over time? | Diminishes |
| 15. What are ADR of higher doses of l-dopa? | Dyskinesia |
| 16. Excessive peripheral dopamine generation in periphery result in what? | ADR |
| 17. How do antiemetics work? | By blocking the dopaminergic receptors in CTZ |
| 18. Why does l-dopa induce N/V? | Because dopaminergic receptors are activated in CTZ induced, which lies outside of BBB |
| 19. What is another ADR of l-dopa? | Postural hypotension due to vasodialation |
| 20. What is IV dopamine called? | Intropin |
| 21. What is low dose intropin known as and why? | 2-5ug/kg/min Renal dose, because it is the dosage that requires to dilate mesenteric, coronary, and renal arteries to increase renal perfusion which leads to diuresis. |
| 22. What receptors does Intropin work on? | D1 – dopamine receptors |
| 23. What is intermediate dose of Intropin? | 5-10ug/kg/min |
| 24. What result in intermediate dose? | Inotropic and chronotropic effect through β1 receptor activation (increased contractility and increased HR) |
| 25. What receptors are stimulated by intermediate dose? | β1 receptor activation |
| 26. What is the high dose Intropin? | 10-20ug/kg/min pressor dose |
| 27. What receptors do high dose Intropin work on? | α1 receptors activated. |
| 28. What result in high dose intropin? | Increase in systemic vasoconstriction and BP shuts down kidneys |
| 29. What are the side effects of Intropin low dose? | Peripheral vasodialation leads to tachycardia and postural hypotension, N/V, Anxiety, agitation, confusion, delusions, hallucinations, depression |
| 30. What ADR do pts have within 2yrs of starting Ldopa Tx? | Dyskinesia, face and limbs |
| 31. What can be done to reduce dyskinesia? | Reduce the l-dopa dose but this will cause rigidity to return |
| 32. What are the other l-dopa related side effects? | Akathesia, psychotic disturbances |
| 33. What can be used to reduce the ADR of peripheral dopamine generation after l-dopa administration? | It can be reduced by use of peripheral decarboxylase inhibitor |
| 34. What is the MOA of Decarboxylase inhibitor? | Block peripheral conversion of L-dopa to Dopamine |
| 35. When inhibiting peripheral dopamine what happens to the l-dopa concentration that crosses BBB? | Increases to 5-10% |
| 36. What is the combination Rx to increase half life of l-dopa therefore decreasing the frequency of administration? | L-dopa+carbidopa |
| 37. What happens when MAO-B is blocked? | Increased dopamine activity |
| 38. Where is MAO-B activity take place? | CNS |
| 39. What is Selegiline? | MAO-B, MonaAmine Oxidase B |
| 40. What is MOA for MAO-B inihibitor (selegiline)? | selectively inhibits MAO-B which metabolizes biogenic amines, reduces dose of l-dopa required by 1/3, reduces the end of dose deterioration in advanced PD |
| 41. What is an ADR of selegiline? | It converts to Amphetamine/Methamphetamin and mess up the sleep wake cycle |
| 42. Is selegiline recommended for monotherapy for PD? | No |
| 43. What is a 2nd generation MAO-B inhibitor that is effective as monotherapy? | Rasagiline because it is not metabolized to amphetamine |
| 44. What are the locations of action of COMT and MAO-B? | Outside of BBB vs. CNS respectively |
| 45. What does COMT(entacapone) do? | Inhibits levodopa degradation and increase half life in periphery, breaks down of 10-30% of l-dopa both peripherally and in the CNS |
| 46. How do peripheral dopa decarboxylase inhibitor (carbidopa) and COMT work together? | COMT (entacapone) is responsible for the metabolism of l-dopa |
| 47. What are the advantages of combination of COMT (entacapone) and dopa decarboxylase inhibitor (carbidopa)? | Double the half life, more l-dopa reaches brain, 50% increase in motor response to each dose of l-dopa |
| 48. How should the l dopa dosage be changed in the presence of entacapone? | Can be reduced |
| 49. What are some properties of entacapone? | Less wear off effect, and does not cross BBB |
| 50. What is Stalevo? | Combination of l-dopa+carbidopa+entacapone |
| 51. When is Stalevo prescribed? | For pts where Sx are not controlled by Sinemet or Madopar (combination of l-dopa+carbidopa) |
| 52. What dopamine receptor agonists cross BBB? | Apomorphine, bromocryptine, lisuride, pergolide, pramipexole, ropinirole act directly on dopamine receptors particularly affect striatum in basal ganglia |
| 53. What happens in long term use of l-dopa Tx in PD? | Motor complications such as abnormal involuntary movements, shortening response to each dose (wear off phenolmenon) |
| 54. What is the role of dopamine agonists? | Reduce the duration of immobile “off” period and the need for l-dopa Tx, and improves motor impairments while only minimally increasing dopaminergic adverse events |
| 55. What result in use of dopamine agonist, Cabergoline? | Dyskenesia and confusion were increased |
| 56. What are the ADRs of dopamine receptor agonists? | N/V, dyskinesia, neuropsychiatric effects with hallucinations and confusion, somnolence and insomnia, gambling, receptor down regulation leading to increased Sx, Fibrotic rxn |
| 57. What dopamine receptor agonists are D2 agonists and ergot alkaloids? | Bromocriptine, Carbergoline, Pergolide |
| 58. What mimics dopamine? | Bromocriptine, which is used to prolactinemia (inhibits prolactin secretion at antipituitary) |
| 59. What receptors do dopamine agonist (Pramipexole) works on? | D1/D3 |
| 60. What are the ADR of Pramipexole? | Nausea, constipation, postural hypotension, somnolence |
| 61. What Rx has high affinity to D4, moderate affinity to D2, D3, D5 adrenoreceptor? | Apomorphine |
| 62. What are some properties of Apomorhpine? | Highly emetogenic, respiratory |
| 63. What are contraindications of Apomorphine? | Co-administration with odasetron (5HT agonist) is contraindicated due to profound hypotension |
| 64. What Rx is effective as monotherapy in early PD and but has to be in combination with l-dopa for later PD? | Amantadine |
| 65. What is MOA for Amantadine? | It is an antiviral Rx that acts by stimulating dopaminergic release and inhibit uptake into nerve terminals. |
| 66. What are some properties of Amantadine? | Tolerance – increased dosage for the same effect, treat dyskinesias, and activity is limited by number of dopamine receptors available |
| 67. What are some antimuscarinic Rx? | Trihexyphenidyl HCk, Benzatropine, Orphenadrine, Procyclidine |
| 68. How do antimuscarinic Rx work? | By blocking central muscarinic receptors and restores balance between cholinergic and dopaminergic activity in the basal ganglia |
| 69. When in antimuscarinic Rx are used? | In advanced PD or when inadequate response to l-dopa |
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sap_213
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