CNS Pharm Final Flashcards by Levi Daugherty

Phenytoin

Uses?
MOA?
Kinetics?

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

How well did you know this?

Not at all

Perfectly

Carbamazepine

Uses?
MOA?
Kinetics?

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

How well did you know this?

Not at all

Perfectly

Ethosuximide

MOA?
Uses?

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

1st line for uncomplicated absence seizures.

No GABA inhibition.

How well did you know this?

Not at all

Perfectly

Valproic acid

Uses?
MOA?
AE?

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!

How well did you know this?

Not at all

Perfectly

Fosphenytoin

Like phenytoin, but more soluble and potent

How well did you know this?

Not at all

Perfectly

Lacosamide

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

How well did you know this?

Not at all

Perfectly

Gabapentin

MOA?
Uses?
AE?

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.

How well did you know this?

Not at all

Perfectly

Pregabalin

MOA?
Uses?
AE?
Metabolism?

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.

How well did you know this?

Not at all

Perfectly

Benzodiazepines as anti epileptics
4 drugs

MOA?
Uses?
AE?

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…

How well did you know this?

Not at all

Perfectly

Vigabatrin

MOA?
Uses?
AE?

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!

How well did you know this?

Not at all

Perfectly

Topical anesthetics: TAC

Uses?

Tetracaine, Epi, and Cocaine

Used for suturing small cuts and wounds.

How well did you know this?

Not at all

Perfectly

Bupivacaine

Uses?
AE?

Used for epidural, but risk of CARDIOTOXICITY

How well did you know this?

Not at all

Perfectly

Ropivacaine

Like bupivicaine, but safer.

How well did you know this?

Not at all

Perfectly

levobupivicaine

AE?

Like bupivicaine, but safer. Less cardiotoxicity.

How well did you know this?

Not at all

Perfectly

Procaine

Uses?
AE?

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

PABA interferes with sulfa drugs.

How well did you know this?

Not at all

Perfectly

Tetracaine

Uses?

Local anesthetic. Spinal and topical uses. High hydrophobicity.

How well did you know this?

Not at all

Perfectly

Lidocaine

Uses?

Most commonly used local anesthetic.

Rapid, and lots of uses.

How well did you know this?

Not at all

Perfectly

Prilocaine

Uses?
AE?

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

Metabolite may cause methemoglobinemia.

How well did you know this?

Not at all

Perfectly

EMLA

What is it?

Eutectic Mixture of Local Anesthetics

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

MAC

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

Meyer overton equation

MAC ~ 1.3/λ
λ=oil/gas coefficient

Potency increases with oil solubility

Ventilation limited drugs
Drugs?
How fast?

Slow induction and recovery

Diethyl ether
Enflurane
Isoflurane
Halothane

Perfusion limited drugs
Drugs?
How fast?

Fast induction and recovery

Nitrous Oxide
Desflurane
Sevoflurane

Balanced anesthesia

N2O + isoflurane

Role of opiates in anesthesia

Used for synergy

Isoflurane AE?

Most popular inhaled anesthetic. Somewhat expensive Potent vasodilator Airway irritant Precipitates myocardial ischemia in pts with CAD

Halothane Uses? AE?

Partial hepatic metabolism Cheap Non-irritant Great for induction in children and maintenance in adults AE is malignant hyperthermia

Nitrous Oxide (N2O) Uses? AE?

Low potency Great for outpatient dentistry and as adjunct to other anesthesia AE is nausea and pneumothorax

Desflurane Use? AE?

Irritant, so better for maintenance rather than induction.

Sevoflurane Use?

Sweet taste, non-irritant Great for pediatric use.

Atracurium

Non-depoarizing blocker Isoquinoline Intermediate acting Releases histamine at high doses

Cisatracurium

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

Gentacurium

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

3 non-depolarizing blockers, intermediate acting

Vecuronium Rocuronium Atracurium

Mecamylamine

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

Non-depolarizing blockers: Major pharmacologic properties

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.

Succinylcholine AE?

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

Disulfiram Use? MOA?

Tx and prevention of alcoholism Inhibits aldehyde dehydrogenase ---> makes you sick! Low pt compliance

Naltrexone Use? MOA?

Tx and prevention of alcoholism Mu receptor antagonist ---> blocks the DA pathways in the CNS

Acamprosate Use? MOA?

Tx and prevention of alcoholism GABA analogue/ weak antagonist of NMDA Probably the best drug for this...

Fomepizole Use? MOA?

Tx for toxicity of Methanol and Ethylene glycol Inhibits Alcohol dehydrogenase, induces P450 ---> increases own metabolism, so dose increase is needed in 48 hours.

Flumazenil Use? MOA?

Tx for BZ or Barbiturate overdose. GABA-A antagonist

Naloxone Use? MOA?

Narcan- Opioid overdose, clinical use Opioid receptor antagonist

Methadone Use?

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

Buprenorphine Use? MOA?

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

Bupropion Uses? MOA? AE?

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.

Verenicline Uses? MOA? AE?

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.