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Neurology > CNS Pharm Final > Flashcards

CNS Pharm Final Flashcards

1
Q

Phenytoin

Uses?
MOA?
Kinetics?

A

Anti epileptic Na+ channel blocker- slows the rate of recovery to the channel resting state. Great for FOCAL and SECONDARILY GENERALIZED seizures, but NOT ABSENCE!

Induces P450, and affects oral contraceptives and a bunch of other stuff.

ZERO order kinetics

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2
Q

Carbamazepine

Uses?
MOA?
Kinetics?

A

Anti epileptic Na+ channel blocker- slows the rate of recovery to the channel resting state. Great for FOCAL and SECONDARILY GENERALIZED seizures, but NOT ABSENCE!

Induces P450, and affects oral contraceptives and a bunch of other stuff including PHENYTOIN.

T1/2 is about 10-20 hours
1st order kinetics

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3
Q

Ethosuximide

MOA?
Uses?

A

T-type Ca++ channel blocker. Great for ABSENCE seizures!

1st line for uncomplicated absence seizures.

No GABA inhibition.

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4
Q

Valproic acid

Uses?
MOA?
AE?

A

Acts on Na+, T-type Ca++, and increases GABA transmission.

Drug of choice for idiopathic generalized, and for absence seizures when ethosuximide isn’t effective. Also an alternate for phenytoin and carbamazepine for focal seizures.

Hepatotoxicity is a major AE—-Tx with L-carnitine

Major teratogen—-spina bifida—-take folate!

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5
Q

Fosphenytoin

A

Like phenytoin, but more soluble and potent

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6
Q

Lacosamide

A

Na+ channel blocker. adjunctive therapy for FOCAL seizures, but with less AE.

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7
Q

Gabapentin

MOA?
Uses?
AE?

A

High voltage Ca++ channel blocker —>decrease in NT release
Used for FOCAL seizures with or without secondary generalization. NOT ABSENCE!

Increase GABA in neural and glial cells, but the anti seizure effect is due to blockage of high voltage Ca++ channels —> decrease in NT release.

Similar to endogenous AAs in structure, so there are very few AE, but its not the most effective, so its not 1st line.

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8
Q

Pregabalin

MOA?
Uses?
AE?
Metabolism?

A

High voltage Ca++ channel blocker —>decrease in NT release
Used for FOCAL seizures with or without secondary generalization. NOT ABSENCE!

Similar to gabapentin, but it works on more stuff such as Glutamate, NE, Substance P, and calcitonin.
More potent than gabapentin.
Adjunct for FOCAL seizures.

*Metabolized by the kidneys, so its ok for liver problem pts.

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9
Q

Benzodiazepines as anti epileptics
4 drugs

MOA?
Uses?
AE?

A

Increases affinity of GABA for GABA-A receptors, leading to an increase of Cl-

Diazepam, Lorazepam, and Midazolam to treat acute FOCAL and TONIC/CLONIC seizures.

Clonazepam inhibits T-type Ca++, so it works on ABSENCE, but due to AE, its 4th line…

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10
Q

Vigabatrin

MOA?
Uses?
AE?

A

GABA analogue irreversibly inhibits GABA transaminase, leading to an increase in GABA. Used for INFANTILE SPASMS and refractory FOCAL epilepsy.

Lots of AE, including bilateral visual field defects and irreversible diffuse atrophy of peripheral retinal nerve fiber layer. —> Pts should get a baseline and routine visual field testing!

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11
Q

Topical anesthetics: TAC

Uses?

A

Tetracaine, Epi, and Cocaine

Used for suturing small cuts and wounds.

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12
Q

Bupivacaine

Uses?
AE?

A

Used for epidural, but risk of CARDIOTOXICITY

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13
Q

Ropivacaine

A

Like bupivicaine, but safer.

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14
Q

levobupivicaine

AE?

A

Like bupivicaine, but safer. Less cardiotoxicity.

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15
Q

Procaine

Uses?
AE?

A

Local anesthetic. Used for infiltration anesthesia and dental procedures, and OB.

PABA interferes with sulfa drugs.

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16
Q

Tetracaine

Uses?

A

Local anesthetic. Spinal and topical uses. High hydrophobicity.

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17
Q

Lidocaine

Uses?

A

Most commonly used local anesthetic.

Rapid, and lots of uses.

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18
Q

Prilocaine

Uses?
AE?

A

Similar to lidocaine, but exhibits vasoconstriction. Nice for when epi is contraindicated.

Metabolite may cause methemoglobinemia.

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19
Q

EMLA

What is it?

A

Eutectic Mixture of Local Anesthetics

Pretty much a combo of lidocaine and prilocaine that is given as a cream or a patch.

20
Q

MAC

A

Minimum Alveolar Concentration

Its a pretty useful sub for Pcns, and its the Palv that results in the lightest anesthesia. Defined as the level that elicits a movement response from 50% of pts on skin incision.

Small MAC = high potency

21
Q

Meyer overton equation

A

MAC ~ 1.3/λ
λ=oil/gas coefficient

Potency increases with oil solubility

22
Q

Ventilation limited drugs
Drugs?
How fast?

A

Slow induction and recovery

Diethyl ether
Enflurane
Isoflurane
Halothane

23
Q

Perfusion limited drugs
Drugs?
How fast?

A

Fast induction and recovery

Nitrous Oxide
Desflurane
Sevoflurane

24
Q

Balanced anesthesia

A

N2O + isoflurane

25
Q

Role of opiates in anesthesia

A

Used for synergy

26
Q

Isoflurane

AE?

A

Most popular inhaled anesthetic.
Somewhat expensive
Potent vasodilator
Airway irritant

Precipitates myocardial ischemia in pts with CAD

27
Q

Halothane

Uses?
AE?

A

Partial hepatic metabolism
Cheap
Non-irritant

Great for induction in children and maintenance in adults

AE is malignant hyperthermia

28
Q

Nitrous Oxide (N2O)

Uses?
AE?

A

Low potency

Great for outpatient dentistry and as adjunct to other anesthesia

AE is nausea and pneumothorax

29
Q

Desflurane

Use?
AE?

A

Irritant, so better for maintenance rather than induction.

30
Q

Sevoflurane

Use?

A

Sweet taste, non-irritant

Great for pediatric use.

31
Q

Atracurium

A

Non-depoarizing blocker
Isoquinoline
Intermediate acting

Releases histamine at high doses

32
Q

Cisatracurium

A

Non-depoarizing blocker
Isoquinoline
Intermediate acting

Most popular muscle relaxant in clinical practice
Uses for pts with impaired renal or hepatic function
Muscle relaxant for Sx and intubation

33
Q

Gentacurium

A

Non-depolarizing blocker
Rapid onset with short duration
Few pulmonary effects

34
Q

3 non-depolarizing blockers, intermediate acting

A

Vecuronium
Rocuronium
Atracurium

35
Q

Mecamylamine

A

Ganglionic blocker used as a possible adjunct to nicotine patch for smoking cessation.

36
Q

Non-depolarizing blockers: Major pharmacologic properties

A

Poor GI absorption
No BBB crossing

*Effects are increased by MYASTHENIA GRAVIS, inhaled anesthetics and AMINOGLYCOSIDE antibiotics.

Effects of drugs are reversed by anticholinesterase agents.

37
Q

Succinylcholine

AE?

A

Depolarizing blocker
Produces fasciculations followed by sustained muscle paralysis

Short duration- preferred choice for intubation.

No antidote in the case of overdose
May cause hyperkalemia in children and muscle soreness in adults.
May cause malignant hyperthermia

38
Q

Disulfiram

Use?
MOA?

A

Tx and prevention of alcoholism

Inhibits aldehyde dehydrogenase —> makes you sick!
Low pt compliance

39
Q

Naltrexone

Use?
MOA?

A

Tx and prevention of alcoholism

Mu receptor antagonist —> blocks the DA pathways in the CNS

40
Q

Acamprosate

Use?
MOA?

A

Tx and prevention of alcoholism

GABA analogue/ weak antagonist of NMDA
Probably the best drug for this…

41
Q

Fomepizole

Use?
MOA?

A

Tx for toxicity of Methanol and Ethylene glycol

Inhibits Alcohol dehydrogenase, induces P450 —> increases own metabolism, so dose increase is needed in 48 hours.

42
Q

Flumazenil

Use?
MOA?

A

Tx for BZ or Barbiturate overdose.

GABA-A antagonist

43
Q

Naloxone

Use?
MOA?

A

Narcan- Opioid overdose, clinical use

Opioid receptor antagonist

44
Q

Methadone

Use?

A

Long acting opioid receptor agonist for the Tx of opioid dependance.

45
Q

Buprenorphine

Use?
MOA?

A

Opioid receptor partial agonist for Tx of opioid dependance. Replaces short acting drugs.

46
Q

Bupropion

Uses?
MOA?
AE?

A

Nicotine addiction Tx

NE and DA reuptake inhibitor; buffers nicotine craving through noncompetitive antagonist activity at alpha-4-beta-2 and alpha-7

lowers seizure threshold.

47
Q

Verenicline

Uses?
MOA?
AE?

A

Nicotine addiction Tx

Partial alpha-4-beta-2 agonist, and full alpha-7 agonist. Use is limited by nausea and insomnia, and is associated with ACUTE PSYCHOSIS and SUICIDAL IDEATION.

Neurology (3 decks)

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