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IPAP Pharmacology 2 > MOAs for Test 4 > Flashcards

MOAs for Test 4 Flashcards

1
Q 
(Lecture 1)
This class of drugs blocks the reuptake of norepinephrine and serotonin (precursors to SNRI) into the presynaptic neuron which increases [monoamine] in the synaptic cleft (debated); also blocks alpha adrenergic, histamine, and muscarinic receptors.
A

Tricyclic Antidepressants

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2
Q

(Lecture 1)
This drug class Inhibits serotonin reuptake, without affecting reuptake of norepinephrine or dopamine into the presynaptic neuron;
they DO NOT SIGNIFICANTLY EFFECT histamine, muscarinic, or other receptors

A

SSRIs

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3
Q

(Lecture 1)

These drugs/classes carry a risk of serotonin syndrome because they INHIBIT SEROTONIN REUPTAKE

A
  • Cocaine
  • Dextromethorphan (DM)
  • Meperidine
  • SSRIs
  • TCAs
  • Trazodone
  • Venlafaxine
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4
Q 
(Lecture 1)
This drug/class carries a risk of serotonin syndrome because it is a DOPAMINE AGONIST
A

L- dopamine

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5
Q 
(Lecture 1)
This drug/class carries a risk of serotonin syndrome because it is a SEROTONIN PRECURSOR
A

L-tryptophan

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6
Q 
(Lecture 1)
These drug/class carries a risk of serotonin syndrome because it INHIBITS SEROTONIN METABOLISM
A

MAOIs

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7
Q

(Lecture 1)

These drugs/classes carry a risk of serotonin syndrome because they INCREASE SEROTONIN RELEASE

A
  • Amphetimines
  • Lithium
  • MDMA (ecstacy)
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8
Q

(Lecture 1)

These drugs/classes carry a risk of serotonin syndrome because they are SEROTONIN RECEPTOR AGONISTS

A
  • Triptans
  • Buspirone
  • Lysergic Acid Diethylamide
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9
Q

(Lecture 1)
This drug class inhibits the reuptake of 5HT and NE, increasing their levels (may be dose-related);
it displays LITTLE activity for alpha-adrenergic, cholinergic, or histamine receptors

A

SNRIs

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10
Q

(Lecture 1)

This drug inhibits dopamine AND Norepinephrine (at high doses) with minimal activity on serotonin

A

Bupropion (an NDRI)

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11
Q

(Lecture 1)
This drug modestly inhibits serotonin uptake (less than SSRIs); are antagonist for pre-synaptic 5HT(2A), H(1), and alpha(1) receptors

A

Trazodone

a serotonin receptor antagonist

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12
Q

(Lecture 1)
This drug inhibits 5HT(2A), H(1), and alpha(1) receptors AND ALPHA 2 receptors, but does not have reuptake inhibition effect.

A

Mirtazapine

a serotonin Receptor Antagonist

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13
Q

(Lecture 1)

This drug inhibits 5HT(2) family of receptors, alpha(1) receptors, and reuptake of serotonin and norepinephrine

A

Nefazodone

a serotonin receptor antagonist

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14
Q 
(Lecture 1)
This drug class blocks the enzyme responsible for the breakdown of NE, dopamine, and serotonin which increases the stores of these neurotransmitters in the neurons
A

MAOIs

Two forms: MAO-A, MAO-B

Foods that interact with these medications occur because they inhibit MAO in the GI tract that normally breaks down tyramine, resulting in increased levels of catecholamines.

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15
Q

(Lecture 1)

These drugs are non-selective MAOIs which are considered last line agents in antidepression

A

Phenelzine

Tranylcypromine

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16
Q

(Lecture 1)
This MAO-B INHIBITOR is used in the treatment of MDD (and Parkinson’s) and claims to exhibit longer time to relapse and less sexual dysfunction and weight gain

A

Selegiline Transdermal System

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17
Q

(Lecture 1)
The MOA of this drug is unknown, but may inhibit 2 signal transduction pathways; it is used in the tx of the manic phase for bi-polar patients and anti-manic effects can occur in 1-2 weeks; it appears to be neuroprotective.

A

Lithium

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18
Q 
(Lecture 2)
This drug class acts directly on postsynaptic dopamine receptors and do not require enzymatic conversion. Specifically, D2 receptor stimulation improves rigidity and bradykinesia in Parkinson's
A

Dopamine agonists

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19
Q

(Lecture 2)

This short-acting dopamine agonist stimulates post-synaptic D2-type receptors

A

Apomorphine

Will probably cause severe N/V… prophylax with trimethobenzamide

20
Q

(Lecture 2)
This Aromatic L-amino Acid Decarboxylase (AAAD) inhibitor DOES NOT CROSS THE BBB; prevents peripheral conversion and metabolism of levopdopa to dopamine in the peripheral tissues, thereby allowing increased availability of levodopa to cross into the CNS

A

Carbidopa

21
Q

(Lecture 2)
This precursor to dopamine HAS THE ABILITY TO CROSS THE BBB and replenish depleted dopamine in the brain; it is CONVERTED TO DOPAMINE IN THE PERIPHERY

A

Levodopa

22
Q

(Lecture 2)
This drug irreversibly inhibits the metabolism of dopamine by MAO-B (ONLY!! -> lower risk of HTN CRISIS) which results in increased dopamine levels in the brain

A

Selegiline

LAST DOSE SOULD BE EARLY AFTERNOON TO PREVENT INSOMNIA

23
Q

(Lecture 2)
This MAOI has not yet had selectivity for MAO-B definitively established, but provides sx relief to PTs suffering from Parkinson’s and has possible neuroprotective effects

A

Rosagiline

  • 5X MORE POTENT THAN SELEGILINE
  • NOT METABOLIZED TO AMPHETAMINE
  • HTN CRISIS POTENTIAL needs ADDITIONAL TESTING
  • DO NOT take with TYRAMINE-containing foods
24
Q

(Lecture 2) This class of drugs blocks the excitatory neurotransmitter ACTH to try and restore balance with dopamine

A

Anticholinergics

EX: Benzatropine; Trihexyphenidyl

25
Q

(Lecture 2)
This NMDA Receptor Inhibitor’s MOA is not completely understood, does not work if dopamine release is already at maximum and has an adverse risk of LIVEDO RETICULARIS

A

Amantadine

26
Q 
(Lecture 2)
This class of drug prevents the dreakdown of dopamine, leaving more levodopa available to cross the BBB
A

COMT Inhibitors

EX: Tolcapone, Entacapone, Stalevo

27
Q

(Lecture 3)
These drugs work by blocking/preventing the spead of electrical discharge by one of several mechanisms:
- Enhancement of GABAnergic transmission
-Diminution of excitatory transmission
-Modification of ionic conductance through ion channels

A

Anticonvulsants

28
Q

(Lecture 3)

This drug is a fast sodium channel blocker used as part of Tx in status epilepticus; DO NOT USE in absence seizures

A

Phenytoin

PREGNANCY CAT D

29
Q

(Lecture 3)
This drug is also a fast sodium blocker and is the PRODRUG for another drug with a similar name and is preferred when parenteral administration is needed

A

Fosphenitoin

1mg PHENYTOIN = 1.5mg FOSPHENYTOIN

30
Q

(Lecture 3)
This drug is a fast sodium channel blocker, a CYP3A4 INDUCER and AUTO-INDUCER, used to tx primary gen. tonic-clonic simple, or complex partial seizures as well as TGN and bipolar disease

A

Carbamazepine

31
Q

(Lecture 3)
This drug is a fast sodium channel blocker, is a CYP inducer, and used similarly to carbamazepine (but less potent) and reserved for PTs who do not tolerate it well

A

Oxcarbazepine

32
Q

(Lecture 3)

This drug’s MOA is to increase GABA mediated chloride influx (inhibitory neurons)

A

Primidone

-IS METABOLIZED TO PHENOBARBITAL AND PHENYLETHYLMALONAMIDE

(Phenobarbital has the same basic MOA)

33
Q

(Lecture 3)
This drug and its derivatives block t-type CALCIUM currents, blocks SODIUM channels, INCREASES GABA PRODUCTION and DECREASES GABA DEGRADATION

A

Valproic acid

34
Q

(Lecture 3)
This drug inhibits the a2delta subunit of voltage-dependent ALCIUM channels and is an analog of GABA, but does not directly impact the GABA receptor

A

Gabapentin

ADEs include DROWSINESS, FATIGUE, DIZZINESS, and WEIGHT GAIN

35
Q

(Lecture 3)
This drug is a GABA derivative similar to Gabapentin that binds pre-synaptically to the a2deltasubunit of the voltage-gated calcium channel AND BLOCKS INFLUX OF Ca2+ IN HYPER-EXCITED NEURONS

A

Pregabalin

ADEs include DIZZINESS and WEIGHT GAIN

36
Q

(Lecture 3)
The way this drug is used is mostly unknown, but is thought to block T-type calcium channels; it is the DOC in absence seizures.

A

Ethosuximide

37
Q

(Lecture 3)
This drug acts by decreasing glutamate and aspartate release, delays repetitive firing of neurons, and blocks fast sodium channels

A

Lamotrigine

38
Q

(Lecture 3)
This drug acts by blocking fast sodium channels, enhancing GABA activity, antagonizing AMPA/kainate activity, and is a weak carbonic anhydrase inhibitor

A

Topiramate

39
Q

(Lecture 3)
This drug binds at voltage gated POTASSIUM CHANNELS and may also exert therapeutic effects through augmentation of GABA-MEDIATED CURRENTS

A

Ezogabine

ADEs include URINARY RETENTION, UTI, QT PROLONGATION, PSYCHOSIS, RETINAL ABNORMALITIES and VISION LOSS (req. periodic vision tests), and SKIN DISCOLORATION

40
Q

(Lecture 3)

This drug works by ENHANCING THE SLOW INACTIVATION OF SODIUM CHANNELS

A

Lacosamide

ADEs include Prolonged PR INTERVAL, AV BLOCKS, MULTIORGAN HYPERSENSITIVITY, NEUTROPENIA

41
Q

(Lecture 3)

This drug IRREVERSIBLY INHIBITS GABA-T and is a MONOTHERAPY FOR INFANTILE SPASMS

A

Vigabactrin

ADEs include VISION LOSS (needs periodic vision testing); RESTRICTED DISTRIBUTION PROGRAM, MRI ABNORMALITIES, DEPRESSION, and WEIGHT GAIN

42
Q

(Lecture 3)

This drug works at BOTH SODIUM AND CALCIUM CHANNELS, is used in the tx of BIPOLAR D/O, and is a SULFONAMIDE

A

Zonisamide

ADEs include RASH, SJS/TEN, APLASTIC ANEMIA, AGRANULOCYTOSIS, NEPHROLITHIASIS

CHILDREN MAY ALSO HAVE FEVER AND HYPERHIDROSIS when using it

43
Q

(Lecture 3)

This drug has WEAK INHIBITORY EFFECTS ON GABA-RECEPTOR BINDING, benzo receptor binding, is a adjunct for Lennox Gastaut

A

Felbamate

ADEs include APLASTIC ANEMIA, LIVER FAILURE

44
Q

(Lecture 3)
This drug ENHANCES THE ACTIVITY OF GABA and is an ADJUNCTIVE therapy for partial seizures, but has a potential ADE of NONCONVULSIVE STATUS EPILEPTICUS

A

Tiagabine

Other ADEs include SJS/TEN

45
Q

(Lecture 3)
This drug is used in the tx of Eclampsia; possibly works by potent cerebral vasodilator properties which reduce the chance of seizures caused by vasospasm decreasing cerebral blood flow

A

MAGNESIUM SULFATE

IPAP Pharmacology 2 (2 decks)

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