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Flashcards in Neuro Drugs Deck (53):
1

Alpha agonists used to treat Glaucoma

Epinephrine (alpha 1) - decreased aqueous humor synthesis via vasoconstriction
Brimonidine (alpha 2) - decreased aqueous humor synthesis

2

S/E of Epinephrine

Mydriasis (alpha 1) --> don't use in acute closed angle glaucoma

3

Mechanism of beta blockers in Glaucoma

Decrease aqueous humor synthesis

4

Acetazolamide mechanism in Glaucoma

Decrease aqueous humor synthesis via inhibition of carbonic anhydrase

5

Direct cholinomimetics used for glaucoma

Pilocarpine, Carbachol

6

Latanoprost (mechanism, use and S/E)

Mech - increases outflow of aqueous humor (a prostaglandin PGF2alpha)
Use - Glaucoma
S/E - Darkens color of iris (browning)

7

Uses of opioids

Pain
Cough suppression
Diarrhea (loperamide, diphenoxylate)
Acute pulmonary edema
Maintenance programs for heroin addicts

8

Butorphanol
a. Mechanism
b. Use
c. Toxicity

a. K opioid agonist and mu opioid partial agonist --> produces anesthesia
b. Severe pain (less resp depression that full agonists)
c. Can cause opioid withdrawal symptoms if patient is also taking full agonist

9

Tramadol
a. Mechanism
b. Use
c. Toxicity

a. Very weak opioid agonist; also inhibits 5-HT and NE reuptake (tram it all = multiple receptors)
b. Chronic pain
c. Decreases seizure threshold, serotonin syndrome

10

Ethosuximide
a. Mechanism
b. Use
c. Toxicity (EFGHIJ)

a. Blocks thalamic T type Ca channels
b. Absence seizures
c. Fatigue, GI distress, Headache, Itching, stevens Johnson syndrome

11

1st line for acute status epilepticus

Benzodiazepines

12

Phenytoin
a. Mechanism
b. Use
c. Toxicity

a. Increases Na channel inactivation; zero order kinetics
b. Prophylaxis of status epilepticus, treatment of simple, complex, tonic-clonic seizures
c. Gingival hyperplasia, hirsutism, megaloblastic anemia, fetal hydantoin syndrome, SLE like syndrome, p-450 induction, Stevens johnson, osteopenia, nystagmus, diplopia, ataxia, sedation

13

Carbamazepine
a. Mechanism
b. Use
c. Toxicity

a. Increases Na channel inactivation
b. Trigeminal neuralgia, simple/complex/tonic-clonic seizures
c. Liver toxicity, Stevens johnson, p-450 inducer, teratogen, SIADH, aplastic anemia, agranulocytosis

14

Valproic acid
a. Mechanism
b. Use
c. Toxicity

a. Increased Na channel inactivation by increasing GABA concentration
b. All seizures, bipolar disorder
c. Hepatotoxic, teratogen

15

Gabapentin
a. Mechanism
b. Use
c. Toxicity

a. Inhibits high voltage activated Ca channels (GABA analog)
b. Simple or complex seizures, peripheral neuropathy or postherpetic neuralgia
c. Sedation, ataxia

16

Phenobarbital
a. Mechanism
b. Use
c. Toxicity

a. Increases GABAa action
b. First line in neonates; simple/complex/tonic-clonic seizures
c. P450 inducer, tolerance, sedation, cardiorespiratory depression

17

Treatment for absence seizure

Ethosuximide, Valproic acid, Lamotrigine

18

Mechanism of barbiturates

Facilitate GABAa action by increasing DURATION of Cl channel opening --> decreased neuronal firing

19

Mechanism of benzodiazepines

Facilitate GABAa action by increased frequency of Cl channel opening

20

Which BDZs have short half life? (ATOM)

Alprazolam
Triazolam
Oxazepam
Midazolam

21

NonBDZ hypnotics

Zolpidem
Zaleplon
EsZopiclone

22

Difference between BDZs and Zolpidem/Zaleplon/Eszopiclone

Less potential for tolerance and addiction
No anticonvulsant properties
No muscle relaxing effects
Not used for anesthesia

23

What affects speed of induction and recovery times?

Decreased solubility in blood = rapid induction and recovery time

24

What determines anesthetic potency?

Inversely proportional to minimal alveolar concentration
Drugs with increased solubility in lipids

25

NO vs. Halothane as anesthetics

NO has low blood and lipid solubility --> fast induction and fast recovery, low potency
Halothane has high blood and lipid solubility --> slow induction/recovery and high potency

26

Which drugs cause malignant hyperthermia (fever and severe muscle contractions)?

Inhaled anesthetics (halothane, enflurane, isoflurane, sevoflurane, methoxyflurance, N2O)
Succinylcholine (neuromusclar blocking drug)

27

Which anesthetics can be used for brain surgery?

Barbiturates are good because they cause decreased cerebral blood flow

28

Ketamine mechanism

Blocks NMDA receptors --> act as dissociative anesthetics
Cardiovascular stimulants, cause disorientation, bad dreams, hallucination

29

Mechanism of local anesthetics

Block Na channels by binding receptors on INNER portion of channel (preferentially bind activated Na channels; tertiary amines penetrate membrane in uncharged form and then bind to ion channels as charged form)

30

Why do you need more local anesthetic in infected tissues?

Infected tissues are acidic and alkaline anesthetics are charged/cannot penetrate membrane effectively

31

What can you give with local anesthetics to enhance action?

Epinephrine (vasoconstrictor)

32

Order of nerve blockade

Small myelinated > small unmyelinated > large myelinated > large unmyelinated

33

Order of loss of sensations with local anesthetic

Pain > temp > touch > pressure

34

What are the local anesthetics?

Esters - Procaine, Cocaine, Tetracaine
Amides - Lidocaine, Mepivicaine, Bupivacaine (two Is in name)

35

What is succinylcholine?

Depolarization neuromuscular blocking drug --> Ach receptor agonist that produces sustained depolarization and inhibits muscle contraction

36

What are the non depolarizing neuromuscular blockers?

Tubocurarine, Atracurium, Mivacurium, Pancuronium, Vecuronium, Rocuronium --> competitive antagonists of Ach nicotinic muscular receptors

37

Baclofen mechanism and use

Inhibits GABAb receptors at spinal cord level --> skeletal muscle relaxation (used for muscle spasms)

38

Cyclobenzaprine mechansim and use

Centrally acting skeletal muscle relaxant used for muscle spasms (Has similar anticholinergic side effects)

39

Dopamine agonists used for Parkinsons

Ergot - Bromocriptine
Non-ergot (preferred) - Pramipexole, Ropinirole

40

Mechanism of Amantadine

Causes increased dopamine release and decreased dopamine reuptake

41

Mechanism of Carbidopa

Prevents peripheral conversion of L-DOPA to dopamine by inhibiting DOPA decarboxylase (reduces peripheral S/E)

42

Mechanism of Entacapone, Tolcapone

Prevent peripheral L-DOPA degradation to 3-O-methyldopa (3-OMD) by inhibiting COMT (Tolcapone also inhibits central COMT but causes hepatotoxicity)

43

Drugs that prevent dopamine breakdown

Selegiline - inhibits MAOb (dopamine not converted to 3-MT)
Tolcapone - blocks conversion of dopamine to DOPAC by inhibiting central COMT

44

Benztropine mechanism

Antimuscarinic that improves tremor in Parkinson patients

45

S/E of L-dopa

Arrhythmias from increased conversion to catecholamines

46

Donepezil

AchE inhibitor used for Alzheimers

47

Galantamine

AchE inhibitor used for Alzheimers

48

Rivastigmine

AchE inhibitor used for Alzheimers

49

Tacrine

AchE inhibitor used for Alzheimers

50

Neurotranmistter changes in Huntingtons

Increased dopamine
Decreased GABA, Ach

51

Treatment for Huntingtons

Tetrabenazine and Reserpine - inhibit VMAT to limit dopamine vesicle packaging and release
Haloperidol - D2 receptor antagonist

52

Triptans
a. Mechanism
b. Use
c. Toxicity

a. 5-HT1b/1d agonists --> induce vasoconstriction, prevent vasoactive peptide release, inhibit trigeminal nerve activation
b. migraine, cluster headache attacks
c. Coronary vasospasm (C/I in patients with Prinzmetal angina and CAD), Mild paresthesia

53

When are triptans C/I?

In patients with prinzmetal angina and CAD, pregnancy