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Neurological System > 3-Pharmacology > Flashcards

3-Pharmacology Flashcards

1
Q

Differentiate among the 3 states of Na+ channels: resting, inactivated, and activated (open). Explain their significance for the generation of action potentials and how anti-epileptics act on them.

A

Resting- hyperpolarized

Active - open transiently in response to membrane depolarization

Inactive - spontaneous closure of the channel

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2
Q

Give 2 types of seizure for which drugs that act via Na+ channel mediated inhibition are NOT used.

A

Phenytoin, Carbemazepine, Valproic Acid, Lamotrigine,

In general, these drugs are strong for focal and secondarily generalized seizures, but NOT absence seizures.

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3
Q

Give the effect of phenytoin and carbamazepine on P450 enzymes

A

They induce P450, and thus decreases the serum levels of other drugs that use P450, namely ORAL CONTRACEPTIVES

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4
Q

Give the type of seizures for which carbemazepine is often used.

A

Focal Seizures

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5
Q

Describe the role of T-type calcium channels in generation of seizures and which category of seizure such drugs work on.

A

Low voltage ca channels used for repetitive type action potentials like the ones in the thalamus during sleep. They are usually inactive when we are awake. If active, can cause absence seizures.

Ethosuxamide and Valproic Acid both indicated for this. SUx is the DOC

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6
Q

Give 3 seizure indications of valproic acid.

A

Very effective in generalized epilepsy, DOC for idiopathic events.

Used as 2nd line for absence seizures

Used as second line for focal seizures too.

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7
Q

Explain how drugs that block high-voltage activated Ca++ channels work and what type of seizure they are NOT used for.

A

Gabapentin and Pregabalin

High voltage channel plays important role in controlling entry into pre-synaptic terminals, thus regulating transmitter release.

Not used for Absence seizures

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8
Q

Explain what population pregabalin is preferred in and why.

A

Hepatically impaired, it is metabolized by the kidneys.

More potent than gabapentin too. Plus it decreases release of other NTs as well. So it has off label uses.

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9
Q

Give three specific benzodiazepines used for focal and tonic-clonic seizures.

A

Lorazepam, Diazepam, Midazolam - usually used to stop acute onset seizures.

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10
Q

Give the mechanism of vigabatrin action as well as two indications for it

A

analog of GABA that inhibits GABA transaminase, increasing levels of GABA in the brain.

Infantile Spasms and Refractory Focal Epilepsy

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11
Q

Give the two initial drugs that can be given for status epilepticus.

A

Benzodiazepines first, followed by phenobarbital if seizures persist

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12
Q

Give the anti-epileptic drug that definitely should NOT be used in pregnant women.

A

Valproic Acid

Carbemazepine too

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13
Q

Explain the role of GABA neurons in surround inhibition

A

Prevent strong APs from activating unintended nearby circuits.

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14
Q

Give two advantages of fosphenytoin over phenytoin.

A

More soluble

More potent

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15
Q

Explain why lacosamide is an alternative to phenytoin and carbemazepine.

A

Binds to NMDA receptors, so it inactivates Na channels via a different route

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16
Q

In spite of their pre-clinical promise explain why none of the specific and potent glutamate receptor antagonists have been routinely used clinically.

A

Behavioral adverse side effects

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17
Q

Describe Felbamate?

A

Glutamate inhibitor used in refractory epilepsy

Can cause aplastic anemia and liver failure.

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18
Q

What is the use of Rufinamide?

A

Refractory epilepsy

Hasn’t shown any serious side effects in trials.

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19
Q

Apply what TAC is and what it is used for to a case scenario

A

Topicals (tetracaine, epinephrine, cocaine)

Applied before suturing small wounds and cuts

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20
Q

Penetration of LAs into the brachial plexus

A

There are many layers of the nerves, and certain nerves are more sensitive than others (Motor fibers last to go). Numbing will exhibit a watershed type numbing proximal to distal.

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21
Q

Potential problem with adding epinephrine to a peripheral nerve block.

A

Used to try and keep the anesthetic contained in the intended area. Can cause hypoxia if it causes too much vasoconstriction

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22
Q

3 Agents used for central nerve block

A

Bupivacaine used for epidurals but may cause cardiotoxicity.

Newer: ropivacaine, levobupivacaine may be safer

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23
Q

Indication for procaine

A

Dental Procedures - infiltration anesthesia

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24
Q

indications for tetracaine

A

Spinal and Topical Anesthesia - slow metabolism

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25
Q

Most commonly used local anesthetic?

A

Lidocaine - all the listed uses are uses for lidocaine - infiltration, PN block, central nerve block, spinal, topical,

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26
Q

Toxic effect of bupivicaine?

A

Cardiotoxicity, might recommend levobupivacaine or ropivacaine.

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27
Q

Components of EMLA and how is it applied?

A

Mixture of lidocaine and prilocaine. Used in a patch or cream for venipuncture procedures, lumbar puncture, dental procedures.

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28
Q

Adverse effect associated with a metabolite of prilocaine

A

Methemglobinemia

29
Q

3 CNS states associated with anesthesia.

A

Loss of consciousness.
Amnesia.
Immobility.

30
Q

Differentiate between the lipid and ion-channel theories of general anesthetics

A

lipid theory: function of excitable membranes is modified by dissolved anesthetics.

ion channels: inhibit excitatory ligand-gated ion channels (nicotinic, NMDA, 5HT3), enhance GABAA and glycine (inhibitory).

31
Q

Explain why Palv is a useful sub. for Pcns?

A

Because Pcns tracks with Palv with only a small time lag

32
Q

Operationally define MAC

A

the Palv that results in the lightest anesthesia.

Defined as Palv that results in movement response to a skin incision in only 50% of patients

33
Q

Apply the Meyer-Overton equation to a clinically-relevant case

A

MAC = 1.3/ (oil/gas) of a drug

SO, sevoflurane = 51lamda

therefore, MAC = 1.3/51 = .025 atm.

Larger the (oil/gas) the more potent the drug is. Because it will cause anesthesia ate a lower Palv

34
Q

Explain the relationship between lamda (oil/gas) and potency and alveolar pressure

A

Larger the (oil/gas) the more potent the drug is. Because it will cause anesthesia ate a lower Palv

35
Q

Give 4 ventilation and 3 perfusion limited anesthetics and their relative induction and recovery times.

A

Ventilation Ltd. - Diethyl ether, enflurane, isoflurane, halothane

Perfusion Ltd. - N2O, desflurane, sevoflurane

36
Q

Apply the most popular anesthetic and the population in which it is contraindicated.

A

Isoflurane - contraindicated in patients with Coronary artery disease.

37
Q

Give 2 advantages of Halothane over isoflurane and one major side effect of it.

A

Low cost
Slow induction and recovery
Adverse - malignant hyperthermia

38
Q

Give 2 uses for N2O

A

Outpatient dentistry

Adjunct to inhaled or IV anesthesia

39
Q

Apply the advantage of sevoflurane in a specific pt. population.

A

Sweeter taste and does not irritate airways. Preferred in children.
Widely used for outpatient anesthesia

40
Q

Apply one example of balanced anesthesia to a clinically-relevant case scenario.

A

Combo of inhaled and IV anesthetics to minimize side effects.

N20/Isoflurane combo

41
Q

Give the uses of opiates in balanced anesthesia.

A

For pain relief and selective control?

42
Q

Special Use for Mecamylamine.

A

Adjunct to nicotine patch against nicotine craving for quitting smoking.

43
Q

3 intermediate-acting, non-depolarizing blockers.

A

Atracurium, cistacurium, rocuronium, and vecuronium.

44
Q

Most popular ganglionic blocker and a particular population its used for

A

Trimethaphan

45
Q

Class of antibiotics that make the effects of non-depolarizing agents more profound

A

Aminoglycosides - gentamycin/streptomycin

46
Q

Mechanistic difference btw non- and depolarizing muscle blockers at the receptor.

A

Non- binds and closes the channel

Dep- leaves it open and blocks

47
Q

List the one depolarizing blocker.

A

Succinylcholine

48
Q

Give one advantage and indication for succinylcholine

A

Airway intubation - muscle relaxation to make it easy to get in.

49
Q

Apply one adverse effect of succinylcholine in adults and in children

A

Kids - hyperkalemia

Adults - cardiac issues

50
Q

Give the effect of Myasthenia Gravis on blocking agents

A

augments the blocking effects of non-depolarizing agents

51
Q

Mechanism of drug addiction

A

activation of mesolimbic-dopaminergic system. Brain reward system

52
Q

Identify drugs that do NOT cause drug addiction

A

Substances that alter perception without causing reward sensation or euphoria

Pure hallucinogens - they target cortical and thalamic circuits

53
Q

Effects of ethanol

A

GABA increases
NMDA inhibition - memory and learning
Indirect cannabinoid activation - dopaminergic/mesolimbic system

54
Q

Side-effects of chronic ehtanol consumption

A

Result from GABA down regulation from overstim. and NMDA up-regulation from understim.

Causing withdrawl sx. (Delerium Tremens), global confusion, delusions, hallucinations, autonomic hyperactivity

Wernicke-Korsakoff syndrome - B1 deficiency(encephalopathy, oculomotor dysfunction, gait ataxia)

55
Q

Pharm of acetominophen and drug-drug interaction with use of ethanol

A

Ethanol plus Acetominophen = increased generation of NAPQI via P450 = toxic to liver

56
Q

Ethanol withdrawl timeline and categories

A

1d - Minor symptoms
2d - Hallucinations
3d - Withdrawl Seizures
4d - Delerium Tremens

57
Q

Drug therapies for ethanol intoxication and prevention of ethanol abuse

A

Disulfriam- not used (enzyme downregulator)

Naltrexone - opiod receptor antagonist - blocks ethanol action on Dopaminergic pathways.

Acamprostate - analog of GABA which blocks mechanisms of ethanol dependence in the brain.

58
Q

Symptoms of methanol and poisoning and treatmetn

A

Methanol - similar to ethanol. snow storm - blindness, gI stress, difficulty breathing

Treat with Fomepizole - inhibitor of ADH

59
Q

Symptoms of ethylene glycol poisoning and treatmetn

A

Excitation followed by depression, metabolic acidosis, oxalate in renal tubules causing insufficiency.

Treat with fomepizole as well.

60
Q

Mechanism for how MDMA, PCP, and LSD cause hallucinations?

A

They all, in some way, decrease inhibitory connections. Which causes overstimulation of the CNS.

MDMA - reversing the action of serotonin reuptake transporters (SERTs), thus releasing a lot.

PCP - blocks NMDA glutamate receptors, thus blocking excitatory transmission for memory and plasticity.

LSD - increase glutamate releast via 5HT2A receptor activation in cerebral cortex

61
Q

Mechanism of GHB, what is it used as?

A

Metabolite of GABA that binds GABAb receptors and causes sedation and amnesia.

62
Q

Treatment plan for barbituate/benzodiazepine overdose?

A

Flumazenil - GABA receptor antagonist

63
Q

3 Treatment strategies for opioid abuse?

A

Naloxone - used for overdose: opiod receptor antagonist

Methadone - long-acting full opoid agonist, as replacement therapy

Buprenophine - long-acting partial opioid agonist, as replacement therapy

64
Q

Three treatment strategies for smoking cessation, what are the best choices for certain scenarios?

A
  1. Nicotine Replacement - curb cravings/withdrawl
  2. Varenicline: partial nicotine agonist - reduce cravings/withdrawl. (DO NOT USE IN patients with psych disorders)
  3. Bupropion: antidepressant, inhibits DA and NE reuptake. Buffer withrawl symptoms. DO nOT USE in patients with history of seizures (lowers threshold)
65
Q

Contrast symptoms of Cocaine, PCP, MDMA, and amphetamine intoxication.

A

Cocaine - paranoid ideations, angina, pupillary dilation.

PCP - nystagmus, shizophrenia symptoms, violence, suicidal behavior, tachycardia

MDMA - hyperthermia, serotonin syndrome, hyperactive bowels, myoclonus, autonomic changes.

Amphetamines - anorexia, hyperthermia, hallucinations,

66
Q

Predict result of interaction between MDMA and MAOIs/

A

Can cause serotonin syndrome (cognitive, autonomic, somatic triad of symptoms. Sometimes death.

67
Q

Differentiate between 3 cannabinoids that may be abused.

A

They all act on GABAergic presynaptic CB1 receptors and inhibit GABA release, resulting in disinhibition, and excitation of VTA neurons.

  1. Tetrahydrocannabinol (THC)- active ingredient in marijuana. CB1
  2. Nabilone - older THC analog, reintroduced as an anti-emetic in cancer treatment
  3. Dronabinol - synthetic THC approved for AIDS related anorexia and prophylaxis for nausea in cancer treatment
68
Q

Categorize drugs of abuse by the targets they act on. (3 categories)

A
  1. G-coupled receptors: opioids, cannabinoids, GHB, LSD/mescaline
  2. Ionotropic receptors: Alcohols, Barbituates/Benzos, Nicotine, PCP
  3. Biogenic amine transporters: Cocaine, Amphetamines, MDMA

Neurological System (10 decks)

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