Drugs with MOAs Flashcards

1
Q

Define the class and mechanism of action of sertraline.

A

SSRI (selective serotonin reuptake inhibitor)

binds to SERT (serotonin reuptake transporters) to increase the length of time serotonin is available in the synaptic cleft.
Also causes desensitization of 5HT-1A receptors on the presynaptic neuron’s dendrites.

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2
Q

Define the class and mechanism of action of fluoxetine

A

SSRI (selective serotonin reuptake inhibitor)

binds to SERT (serotonin reuptake transporters) to increase the length of time serotonin is available in the synaptic cleft.
Also causes desensitization of 5HT-1A receptors on the presynaptic neuron’s dendrites.

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3
Q

Define the class and mechanism of action of citalopram

A

SSRI (selective serotonin reuptake inhibitor)

binds to SERT (serotonin reuptake transporters) to increase the length of time serotonin is available in the synaptic cleft.
Also causes desensitization of 5HT-1A receptors on the presynaptic neuron’s dendrites.

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4
Q

Define the class and mechanism of action of trazodone.

A

SSRI (selective serotonin reuptake inhibitor)

binds to SERT (serotonin reuptake transporters) to increase the length of time serotonin is available in the synaptic cleft.
Also causes desensitization of 5HT-1A receptors on the presynaptic neuron’s dendrites.

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5
Q

Define the class and mechanism of action of escitalopram.

A

SSRI (selective serotonin reuptake inhibitor)

binds to SERT (serotonin reuptake transporters) to increase the length of time serotonin is available in the synaptic cleft.
Also causes desensitization of 5HT-1A receptors on the presynaptic neuron’s dendrites.

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6
Q

What are SSRI’s used to treat?

A

depression (MMD and bipolar)

obsessive compulsive disorder

panic disorder

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7
Q

Define the class and mechanism of action of protripytline.

A

Tricycline Secondary Amine Antidepressant

Is a non-selective NET inhibitor (also blocks SERT, sodium channels, muscarinic receptors, and histamine 1 receptors)
- the secondary amine in these is what gives it selectivity for NET

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8
Q

Define the class and mechanism of action of nortriptyline.

A

Tricycline Secondary Amine Antidepressant

Is a non-selective NET inhibitor (also blocks SERT, sodium channels, muscarinic receptors, and histamine 1 receptors)
- the secondary amine in these is what gives it selectivity for NET

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9
Q

Define the class and mechanism of action of desipramine.

A

Tricycline Secondary Amine Antidepressant

Is a non-selective NET inhibitor (also blocks SERT, sodium channels, muscarinic receptors, and histamine 1 receptors)
- the secondary amine in these is what gives it selectivity for NET

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10
Q

Define the class and mechanism of action of maprotiline.

A

Tricycline Secondary Amine Antidepressant

Is a non-selective NET inhibitor (also blocks SERT, sodium channels, muscarinic receptors, and histamine 1 receptors)
- the secondary amine in these is what gives it selectivity for NET

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11
Q

Define the class and mechanism of action of atomoxetine.

A

Tricycline Secondary Amine Antidepressant

Is a non-selective NET inhibitor (also blocks SERT, sodium channels, muscarinic receptors, and histamine 1 receptors)
- the secondary amine in these is what gives it selectivity for NET

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12
Q

Define the class and mechanism of action of nisoxetine.

A

Non-tricyclic Secondary Amine NRI (norepinephrine reuptake inihbitor)

Has a methoxy group that restricts its conformation so that it is selective for NET (norepinephrine reuptake transporter) instead of SERT

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13
Q

Define the class and mechanism of action of imipramine.

A

Tertiary Amine SNRI (serotonin-norepinephrine reuptake inhibitor)

Increases levels of both 5-HT (serotonin) and norepinephrine in the synaptic cleft by blocking both SERT and NET channels

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14
Q

Define the class and mechanism of action of amitriptyline.

A

Tertiary Amine SNRI (serotonin-norepinephrine reuptake inhibitor)

Increases levels of both 5-HT (serotonin) and norepinephrine in the synaptic cleft by blocking both SERT and NET channels.
The propylideneamine moiety makes it sensitive to light.

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15
Q

Define the class and mechanism of action of clomipramine.

A

Tertiary Amine SNRI (serotonin-norepinephrine reuptake inhibitor)

Increases levels of both 5-HT (serotonin) and norepinephrine in the synaptic cleft by blocking both SERT and NET channels.
Most potent because of how preferentially it blocks SERT.

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16
Q

Define the class and mechanism of action of trimipramine.

A

Tertiary Amine SNRI (serotonin-norepinephrine reuptake inhibitor)

Increases levels of both 5-HT (serotonin) and norepinephrine in the synaptic cleft by blocking both SERT and NET channels

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17
Q

Define the class and mechanism of action of doxepin.

A

Tertiary Amine SNRI (serotonin-norepinephrine reuptake inhibitor)

Increases levels of both 5-HT (serotonin) and norepinephrine in the synaptic cleft by blocking both SERT and NET channels

18
Q

Define the class and mechanism of action of venlafaxine.

A

Noncyclic SNRI (serotonin-norepinephrine reuptake inhibitor)

Works like a normal tricyclic SNRI (blocks SERT and NET), but changing it to be non-cyclic removed unwanted adverse effects of the tricyclic inhibitors.

Venlafaxine is 30 times more potent at blocking SERT than NET, and the metabolite is equally potent.

19
Q

Define the class and mechanism of action of duloxetine.

A

Noncyclic SNRI (serotonin-norepinephrine reuptake inhibitor)

Works like a normal tricyclic SNRI (blocks SERT and NET), but changing it to be non-cyclic removed unwanted adverse effects of the tricyclic inhibitors.

Duloxetine exhibits dual inhibition with high affinity for both SERT and NET, with a five-fold preferential for SERT.

20
Q

Define the class and mechanism of action of bupropion.

A

Selective inhibitor of dopamine reuptake at the dopamine presynaptic neuronal membrane and is an NRI (norepinephrine reuptake inhibitor)
(increased by DA and NE)

Also functions as a nicotinic acetylcholine receptor inhibitor underlying various nicotinic effects and cravings associated with smoking cessation, so it can reduce withdrawal symptoms.

21
Q

Define the class and mechanism of action of tranylcypromine and moclobemide.

A

Monoamine oxidase inhibitors.

Mostly used in atypical depression and bulimia (off-label).

22
Q

Define the class and mechanism of action of lithium.

A

Mood stabilizer.

Blocks signal transduction pathways. An important one involves inositol triphosphate (IP3). Normally it would be involved in neuronal signaling associated with neural activation, so blocking this reduces the amplitude of mood changes.

Lithium is specific to the CNS because inositol can’t cross the BBB and replenish the levels that have been depleted by lithium.

23
Q

Define the class and mechanism of action of methotrexate.

A

Immunosuppressant.

Prevents proliferation of immune cells.

24
Q

Define the class and mechanism of action of cyclophosphamide.

A

Immunosuppressant.

Prevents proliferation of immune cells.

Used in treatment of secondary progressive form of MS.

25
Q

Define the class and mechanism of action of propranolol.

A

Non-selective beta blocker

26
Q

Define the class and mechanism of action of practolol.

A

B1 selective beta blocker (first cardio-selective beta blocker)

27
Q

Define the class and mechanism of action of esmolol.

A

Short-acting beta blocker

indicated for use in intraoperative or postoperative tachycardia or hypertension

28
Q

Define the class and mechanism of action of pindolol

A

Beta blocker

has an indole ring that makes it unique

29
Q

Define the class and mechanism of action of timolol.

A

Beta blocker

has a polar heterocyclic ring (thiadiazol-morpholino group) that reduces the log-P value

30
Q

Define the class and mechanism of action of lisinopril.

A

ACE Inhibitor

Antihypertension agent; developed based on how another metalloproteinase enzyme is inhibited.

31
Q

Define the class and mechanism of action of enalapril.

A

ACE Inhibitor

is a prodrug of enalaprilat

32
Q

Define the class and mechanism of action of aliskiren.

A

Renin inhibitor

is a transition state analogue that mimics the tetrahedral geometry of the reaction intermediate

33
Q

Define the class and mechanism of action of lovastatin, pravastatin, and simvastatin.

A

They are Type 1 Statins

Work as an HMG-CoA reductase inhibitor to prevent the formation of cholesterol.

Statins are technically transition state analogues because they mimic the transition state of the first reduction step (there are two reductions, both of which involve NADPH in the normal reaction).

These three all contain asymmetric centers and are harder to synthesize.

Lovastatin and Simvastatin are prodrugs.

34
Q

Define the class and mechanism of action of fluvastatin, atorvastatin, rosuvastatin, and cerivastatin.

A

Type 2 Statins (HMG-CoA reductase inhibitor)

are all synthetic agents that contain a larger hydrophobic moiety than type 1 statins and they don’t have asymmetric centers so they’re easier to synthesize.

Rosuvastatin is very potent because of its sulfonamide group.

35
Q

Define the class and mechanism of action of levodopa (+carbidopa)

A

Dopamine replacement therapy.

L-dopa precursor (levodopa) with a decarboxylase inhibitor (carbidopa) to prevent the L-dopa from being decarboxylated to the active form outside of the CNS.

36
Q

Define the class and mechanism of action of pramipexole and ropinirole.

A

D2 agonists (Dopamine 2 receptor)

Limits the fluctuations in response to L-dopa and prolongs dopaminergic action

37
Q

Define the class and mechanism of action of flupirtine.

A

Non-opioid non-NSAID analgesic

It blocks the chain that is induced by bradykinin
- binds to potassium channels, preventing them from opening, and thus blocking the production of the pain response

Used in headaches, musculoskeletal pain, neurogenic pain, cancer pain, fibromyalgia, and post-operative pain

Advantages: no side effects of NSAIDs and opioids

Interacts with warfarin and can increase toxicity

38
Q

Define the class and mechanism of action of amitiza.

A

Chloride channel activator

Indicated in the treatment of chronic idiopathic constipation in adults OR the treatment of IBS-C

MOA: activates chloride channels to enhance chloride-rich intestinal fluid secretion.
- this increases the motility of the intestine, facilitating the passage of stool and alleviating symptoms associated with chronic idiopathic constipation

39
Q

Define the class and mechanism of action of Linzess (linaclotide).

A

Guanylate Cyclase-C agonist (GC-C)

indicated for treatment of idiopathic constipation OR IBS-C

activation of GC-C results in an increase in both intracellular and extracellular cGMP, stimulating secretion of chloride and bicarbonate into the intestinal lumen
- results in increased intestinal fluid and accelerated transit

40
Q

Define the class and mechanism of action of Plecanatide (Trulance).

A

Guanylate Cyclase-C (GC-C) agonist

indicated for treatment of chronic idiopathic constipation.

activation of GC-C results in an increase in both intracellular and extracellular cGMP, stimulating secretion of chloride and bicarbonate into the intestinal lumen
- results in increased intestinal fluid and accelerated transit

41
Q

Define the class and mechanism of action of docusate (colase).

other names include ex-lax and senokot S

A

Laxative of the Stool Softener Type

Indicated for use in constipation

Is an anionic surfactant

  • lowers the surface tension at the oil-water interface of the feces, allowing water and lipids to penetrate the stool
  • this helps hydrate and soften the fecal material, facilitating natural defecation
42
Q

Define the class and mechanism of action of ondansetron (zofran).

A

5-HT3 Antagonist

Indicated for prevention of nausea and/or vomiting.

MOA not fully characterized, but serotonin receptors (of the 5-HT3 type) are present both peripherally on the vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema