First Aid: Neuro Pharm

Front 1

Glaucoma drugs: classes and specific drugs

Back 1

1. alpha agonists: epinephrine, brimonidine

2. beta blockers: timolol, betaxolol, careolol

3. diuretics: acetazolamide

4. cholinomimetics:
direct: carbachol, pilocarpine
indirect: physostigmine, echothiophate

5. prostaglandin: latanoprost

Front 2

Glaucoma - Epinephrine

Back 2

decrease aq humour synthesis through vasoconstriction
mydriasis, stinging

[DO NOT USE in closed angle glaucoma]

Front 3

Glaucoma - Brimonidine

Back 3

alpha-agonist, decreases aq humor synthesis

[no side effects]

Front 4

Glaucoma - Beta blockers

Back 4

decrease aq humour secretion
timilol, betaxolol, carteolol

[no side effects]

Front 5

Glaucoma - Acetazolamide

Back 5

decrease aq humour secretion by decreasing HCO3- via inhibition of carbonic anhydrase

[no side effects]

Front 6

Glaucoma - Cholinomimetics

Back 6

Increase outflow of aq humour, contract ciliary muscle (which produces aq humour) and opens trabecular network into canal of Schlemm

[miosis, cyclospasm (accomodate)]

Front 7

Which glaucoma drug do you use in an emergency?

Back 7

Pilocarpine

Front 8

Glaucoma - Latanoprost

Back 8

Prostaglandin (PGFa2), increase outflow of aq humour

[Darkens iris (browning)]

Front 9

Opioid analgesics - drugs

Back 9

Morphine
Fentanyl
Codeine
Heroin
Methadone
Meperidine
Dextromethorphan

Front 10

Opioid analgesics - mechanism

Back 10

Agonist at opioid receptors, mu (morphine), delta (enkephalin), kappa (dynorphin)
Open K close Ca channels --> decrease synaptic transmission

Inhibit release of ACh, NE, 5HT, glutamate, substance P

Front 11

Opioid analgesics - use

Back 11

Pain
Cough suppression (dextromethorphan)
Diarrhea (loperamide and diphenoxylate)
Acute pulmonary edema
Maintenance program for addicts (methadone)

Front 12

Which opioid is used for cough suppression?

Back 12

Dextromethorphan

Front 13

Which opioids are used for diarrhea?

Back 13

Loperamide and diphenoxylate

Front 14

Which opioids are used for maintenance in drug addicts?

Back 14

Methadone

Front 15

Toxicity of opioid analgesics

Back 15

Tolerance
Respiratory depression
Constipation
Miosis
CNS depression with other drugs

Front 16

What do you treat opioid toxicity with?

Back 16

Opioid receptor antagonists:
naltrexone
naloxone

Front 17

What do you NOT develop tolerance to when using opioids?

Back 17

Miosis
Constipation

Front 18

Butorphanol

Back 18

Partial agonist at opioid mu receptors, agonist at kappa
Use: Pain, causes less respiratory depression than full agonists

[Causes withdrawal if on full agonists]

Front 19

Which opioid causes less respiratory depression in comparison to other opioids?

Back 19

Butorphanol

Front 20

Tramadol

Back 20

Weak opioid agonist, inhibits Serotonin and NE reuptake (works on multiple neurotransmitters)
Use: chronic pain

[decreases seizure threshold]

Front 21

Phenytoin
(Parenteral: fosphenytoin)

Back 21

Simple Partial, Simple Complex
1st line for Generalized Tonic-Clonic, 1st line Prophylaxis for Status

Use dependent blockade of Na+ channels, decrease refractory period, inhibit glutamate release form excitatory presynaptic neurons

Front 22

Phenytoin toxicity

Back 22

Gingival hyperplasia in kids
Hirsutism
Megaloblastic anemia (decreases folate absorption)
Teratogenesis (fetal hydantoin syndrome)
SLE-like syndrome
CYP450 inducer

Front 23

Carbamezapine

Back 23

1st line for all Simple Partial, Simple Complex, Generalized Tonic-Clonic

Increases Na channel inactivation

Front 24

Which drug is 1st line for trigeminal neuralgia?

Back 24

Carbamezapine

Front 25

Lamotrigine

Back 25

PS, PC, GTC

Blocks voltage-gated Na channels

Front 26

Gabapentin

Back 26

PS, PC, GTC

GABA analogue, but MOA: blocks high voltage activated Ca channels

Front 27

Topiramate

Back 27

PS, PC, GTC

Blocks Na channels, increases GABA action

Front 28

Phenobarbital

Back 28

PS, PC, GTC

Increases duration of Cl- channel opening, increases GABA action

Front 29

Which AED is the first line for kids and pregnant women?

Back 29

Phenobarbital

Front 30

Which drugs are first line for GTC seizures?

Back 30

Phenytoin
Carbamezapine
Valproic acid

Front 31

Valproic acid

Back 31

PS, PC, 1st line for GTC

Increase Na inactivation, increase GABA action

Front 32

Which AED is also used for myoclonic seizures?

Back 32

Valproic acid

Front 33

Ethosuximide

Back 33

1st line for absence seizures

Block Ca channels in thalamus

Front 34

Benzo's

Back 34

first line for acute status epilepticus

increase frequency of Cl- channel opening

Front 35

Tiagabine

Back 35

PS, PC

inhibit GABA reuptake

Front 36

Vigabatrin

Back 36

PS, PC

inhibits GABA transaminase, increasing GABA

Front 37

Levetiracetam

Back 37

PS, PC, GTC

Unknown

Front 38

Which AEDs are first line for status epilepticus?

Back 38

Prophylaxis: Phenytoin

Acute: Benzo

Front 39

Which AED is used for seizures in eclampsia?

Back 39

Benzo

MgSO4 is first line

Front 40

What are the only drugs for absence seizures?

Back 40

ethosuximide is first line for absence
valproic acid can be used

Front 41

Benzodiazepine toxicities

Back 41

Sedation
Tolerance
Dependance

Front 42

Carbamezapine toxicity

Back 42

Blood dyscrasias (aplastic anemia and agranulocytosis)
Liver toxicity
Teratogenesis
CYP450 inducer
SIADH
Stevens-Johnsons syndrome

Front 43

Ethosuximide toxicity

Back 43

"EFGH"
Ethosuximide: Fatigue, GI Distress, Headaches
Stevens-Johnsons syndrome

Front 44

Stevens-Johnsons syndrome

Back 44

Prodrome of malaise and fever
Rapid onset erythematous/purpuric macules (oral, ocular, genital)
Epidermal necrosis and sloughing

Ethosuximide, Carbamezapine, Lamotrigine, Phenytoin, Phenobarbital

Front 45

Phenobarbital toxicity

Back 45

Sedation
Tolerance/Dependance
CYP450 inducer

Front 46

Valproic acid toxicity

Back 46

GI distress, Fatal hepatotoxicty, NTDs/spina bifida in fetus, Tremor, Weight gain

C/i in pregnancy

Front 47

Lamotrigine toxicity

Back 47

Stevens-Johnsons syndrome

Front 48

Gabapentin toxicity

Back 48

Sedation
Ataxia

Front 49

Topiramate toxicity

Back 49

Sedation, Mental dulling, Kidney stone, Weight loss

Front 50

Barbiturates

Back 50

Phenobarbital, Thiopental
Use: Anxiety, seizures, induction for anesthesia

[Additive CNS depression, respiratory/CV depression, Induction of CYP450]
OD: assist respiration and increase BP

Front 51

Which AED is c/i in porphyria?

Back 51

Barbiturates

Front 52

Benzodiazepines

Back 52

anxiety, spasticity, epilepticus, detox from EtOH, night terrors, sleep walking, general anesthetic, hypnotic

[dependence, additive CNS depression with EtOH, less risk of respiratory depression and coma than with barbiturates]

Front 53

How do you Tx benzo overdose?

Back 53

Flumazenil

GABA receptor antagonist

Front 54

Which benzo's have the highest addictive potential?

Back 54

TOM-thumb is Short acting

Triazolam, Oxazepam, Midazolam

Front 55

How do CNS drugs cross BBB?

Back 55

1. soluble in lipid

OR

2. transporter

Front 56

Drugs with decreased solubility in the blood have:

Back 56

rapid induction and recovery times

Front 57

Drugs with increased solubility in lipids have:

Back 57

Increased potency = 1/MAC

MAC = minimal alveolar concentration @ which 50% of population is anesthetized

Front 58

Halothane has increased blood and lipid solubility, what does this mean in terms of potency and induction?

Back 58

increased blood solubility: slow induction
increased lipid solubility: high potency

Front 59

Mechanism of anesthetic action in lungs

Back 59

increases rate and depth of ventilation

Front 60

Mechanism of anesthetic action in blood

Back 60

increased blood solubility: increase gas required to saturate blood --> slow induction time

Front 61

Mechanism of anesthetic action in tissue (i.e. brain)

Back 61

increased solubility: increased gas required to saturate tissue --> slower onset of action

Front 62

Inhaled anesthetics

Back 62

Halothane, isoflurane, nitrous oxide

myocardial and respiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand)

Hepatotoxicity - halothane
Nephrotoxicity - methoxyflurane
Proconvulsant - enflurane
Malignant hyperthermia (all but N2O)

Front 63

IV anesthetics (5)

Back 63

BBKing on OPIATES PROPoses FOOLishly

Barbiturates, Benzodiazepine, Ketamine, Opiates, Propofol

Front 64

Thiopental

Back 64

IV anesthetic, barbiturate

high potency, high lipid solubility, rapid entry into brain
induction anesthesia, short surgical procedures
effect terminated by rapid redistribution into fat and tissues
DECREASES cerebral blood flow

Front 65

Midazolam

Back 65

IV anesthetic, midazolam most commonly used for endoscopy
adjunctively with gas anesthetics and narcotics
severe post-op respiratory depression, amnesia, decreases BP

Front 66

Ketamine

Back 66

PCP, dissociative anesthesia
blocks NMDA receptors
Cardiovascular stimulant
INCREASES cerebral blood flow

Front 67

Opiates used as IV anesthetics

Back 67

Morphine, fentanyl

Front 68

Propofol

Back 68

IV rapid induction of anesthesia, short procedures
potentiates GABA
Less post-op nausea than thiopental

Front 69

Ester local anesthetics

Back 69

Procaine, cocaine, tetracaine
only 1 "i"

Front 70

Amide local anesthetics

Back 70

lidocaine, mepivacaine, bupivacaine
(amides have 2 i's each)
use these if allergic to Esters

Front 71

Local anesthetics: mechanism

Back 71

block Na channels

binds better to activated Na channels, so most effective in rapidly firing neurons

Front 72

Tertiary local amides penetrate membrane in what form and bind to ion channels in what form?

Back 72

penetrate in uncharged
bind in charged form

Front 73

In infected (acidic) tissue, how must local anesthetics be administered differently?

Back 73

Alkaline anesthetics are charged and can't penetrate acidic membrane effectively, so must administer more

Front 74

Order of nerve blockade in local anesthetics

Back 74

Size factor predominates over myelination.
small myelinated > small unmyelinated > large myelinated > large unmyelinated

Front 75

Order of sensory loss in local anesthetics

Back 75

Pain > Temperature > Touch > Pressure

Front 76

Local anesthetics are usually given with what drug and why?

Back 76

Vasoconstrictors (Epi), they enhance local action

*except cocaine

Front 77

NMJ blockers

Back 77

muscle paralysis in surgery or mechanical ventilation
Motor nicotinic
Depol (Succinylcholine) and Non-depol (Tubocurarine, Atracurium, etc)

Front 78

Local anesthesia toxicity

Back 78

CNS excitation
Severe CV toxicity (bupivacaine)
HTN, Hypotension, Arrhythmias (cocaine)

Front 79

Succinylcholine

Back 79

strong ACh Nicotinic (NMJ) receptor AGONIST --> sustained depolarization & prevents muscle contraction.

Phase 1: prolonged depol, no antidote (block POTENTIATED by AChE inhibitors!)
Phase 2: repolarized but blocked, can reverse with AChE inhibitor (neostigmine)

[Hypercalemia, Hypercalcemia, Malignant Hyperthermia]

Front 80

Non-depolarizing NMJ blockers

Back 80

tubocurarine, atracurium, pancuronium, etc
competitive ANTAGONISTS for ACh

Reverse with: AChE inhibitors (neostigime, edrophonium)

Front 81

Dantrolene

Back 81

tx for Malignant Hyperthermia and Neuroleptic Malignant Syndrome

prevents release of Ca from sarcoplasmic reticulum of skeletal muscle

Front 82

Malignant hyperthermia is caused by

Back 82

Inhalational anesthetics (except N2O)
Succinylcholine (depolarizing strong ACh nicotinic AGONIST)

Front 83

Parkinson's has excess____ activity

Back 83

cholinergic due to loss of dopaminergic neurons

Front 84

PD drug classes

Back 84

1. dopamine agonists - Bromocriptine

2. drugs that increase dopamine - Amantadine, L-dopa/carbidopa

3. prevent dopamine breakdown - Selegiline

4. decrease cholinergic activity - Benztropine

Front 85

Parkinson's Drugs - BALSA

Back 85

Bromocriptine
Amantadine
Levodopa/Carvidopa
Selegiline
Anti-muscarinics

Front 86

Parkinson's Disease:
Dopamine agonists

Back 86

Bromocriptine (ergot)
Pramipexole, Ropinirole (non-ergot, preferred)

Front 87

Parkinson's Disease:
Amantadine

Back 87

Increases dopamine release
also used as antiviral against influenza A & rubella

[ataxia]

Front 88

Parkinson's Disease:
Selegiline

Back 88

selective MAO-B inhibitor, which prefers metabolism of dopamine instead of NE or 5-HT
adjunct to L-dopa

[may enhance adverse effects of L-dopa]

Front 89

Parkinson's Disease:
Benztropine

Back 89

anti-muscarinic, improves tremor and rigidity, but little effect on bradykinesia

Front 90

L-Dopa/carbidopa toxicity

Back 90

arrhythmias from peripheral conversion of L-dopa --> increased catecholamines

[Long-term: "Wearing off effect" after 3-5yrs: dyskinesia after administration & akinesia between doses]

Front 91

Why is carbidopa given in PD?

Back 91

peripheral decarboxylase inhibitor

decreases peripheral side effects of L-dopa and increases bioavailability in brain

Front 92

Alzheimer's Disease drugs

Back 92

Memantine (NMDA receptor ANTAGONIST)

Donepezil, Galantamine, Rivastigmine (AChE inhibitors)

Front 93

Huntington's drugs

Back 93

Tetrabenazine, Reserpine (inhibit VMAT)

Haloperidol (dopamine receptor ANTAGONIST)

Front 94

Sumatriptan

Back 94

5-HT agonist. Causes vasoconstriction, inhibits trigeminal activation and vasoactive peptide release.
half-life <2hrs
Acute migraine and cluster HAs

[Coronary vasospasm (contraindicated in CAD or Prinzmetal's angina), mild tingling]

Front 95

Donepezil, Galantamine, Rivastigmine

Back 95

Alzheimer's:
AChE inhibitors

[Nausea, dizziness, insomnia]

Front 96

Memantine

Back 96

Alzheimer's:
NMDA receptor ANTAGONISTS
helps prevent excitotoxicity (mediated by Ca2+)

[Dizziness, confusion, hallucinations]

Front 97

Tetrabenazine

Back 97

Huntington's:
inhibits VMAT --> limits dopamine vesicle packaging & release

Front 98

Reserpine

Back 98

Huntington's:
inhibits VMAT --> limits dopamine vesicle packaging & release

Front 99

Haloperidol

Back 99

Huntington's:
Dopamine receptor antagonist