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FM1 > Pharm Block 2 MOA > Flashcards

Pharm Block 2 MOA Flashcards

1
Q

Prednisone

A

Prodrug of prednisolone, metabolized in vivo to prednisolone

Acts via nuclear receptors to modulate gene expression

Anti-inflammatory: represses COX-2 expression; decrease cytokine production; decreased formation and release of endogenous inflammatory mediators; causes apoptosis of eosinophils

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2
Q

Cyclosporine

A

Calcineurin inhibitor (CNI)

Binds to CYCLOPHILIN, complex binds to calcineurin and inhibits phosphatase activity. Prevents dephosphorylation and translocation of transcription factor NF-AT (stimulates cytokine gene expression)

Inhibits T cell activation and decreased levels of Il-2, IL-3, IL-4, TNF-alpha, IFN-gamma

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3
Q

Tacrolimus

A

Calcineurin inhibitor (CNI)

Forms complex with FK BINDING PROTEIN, complex binds to calcineurin and inhibits phosphatase activity. Prevents dephosphorylation and translocation of transcription factor NF-AT (stimulates cytokine gene expression)

50-100X MORE POTENT THAN CYCLOSPORINE

Inhibits T cell activation and decreased levels of Il-2, IL-3, IL-4, TNF-alpha, IFN-gamma

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4
Q

Sirolimus

A

Binds to FK binding protein, FKBP binds to mTOR to inhibit mTORC1 complex (key kinase involved in upstream regulation of protein synthesis, cell growth, proliferation
Inhibits progression from G1 –> S

Cytostatic: T cells still produce IL-2 but fail to proliferate

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5
Q

Azathioprine

A

Azathioprine -> 6-MP -> 6-thioguanine -> 6-thioguanine nucleotides (incorporated into DNA and RNA -> impaired function)

6-MP and 6-thioguanine also interfere with enzymes of purine nucleotides, decreased ATP and GTP, decreased glycoproteins

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6
Q

Mycophenolate mofetil

A

Mycophenolic acid is reversible inhibitor of inosine monophosphate dehydrogenase, inhibits the de novo pathway of guanosine biosynthesis that is critical to lymphocyte proliferation and activation, results in blunted T and B cell responses

Selective for lymphocytes; other cells are able to recover purines via a separate salvage pathway and can escape the effect

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7
Q

Muromonab-CD3

A

Binds T cell receptor-associated CD3 complex, causes initial activation and cytokine release, followed by blockade, apoptosis, and depletion of T cells

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8
Q

Basiliximab

A

IL-2 receptor antagonist; binds with high affinity (Kp 0.1 nM) to CD25, the IL-2 receptor alpha chain on activated T cells, preventing binding of and signaling by IL-2

CD25 is only expressed on activated T cells, so basiliximab does not cause widespread T cell depletion

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9
Q

Adalimumab

A

Binds TNF-alpha preventing its interactions with p55 and p75 cell surface TNF receptors; decreases biological activity of TNF-alpha

Clinical response is decreased levels of pro-inflammatory cytokines such as IL-1 and IL-6, decreased leukocyte migration, decreased activation of neutrophils and eosinophils, decreased fibroblast proliferation, decreased synthesis of prostglandins, decreased matrix metalloproteinases that produce tissue remodeling responsible for cartilage destruction

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10
Q

Carbachol

A

Agonist at muscarinic receptors; significant NicotinicN receptor activity

Constricts the iris and ciliary body resulting in reduction in IOP

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11
Q

Methacholine

A

Agonist at muscarinic receptors; slight nicotinic activity

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12
Q

Bethanechol

A

Muscarinic agonist with no nicotinic activity

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13
Q

Pilocarpine

A

Muscarinic agonist

Contracts ciliary and circular muscles resulting in miosis and increased flow of aqueous humor in open-angle glaucoma

Closed-angle glaucoma miosis opens anterior chamber of the eye through which aqueous humor exits

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14
Q

Nicotine

A

Agonist at Nm and Nn receptors

Complex action, affects CNS and all branches of PNS

Stimulates catecholamine release from adrenal medulla

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15
Q

Varenicline

A

High-affinity partial agonist at alpha4beta1 nicotinic receptors

Moderate affinity at 5-HT3 receptors

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16
Q

Physostigmine

A

Competes with ACh for its binding site on AChE
Carbamoylates AChE, inactivating it for extended periods of time (increase ACh)

Actions mimic cholinergic stimulation

Crosses BBB

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17
Q

Neostigmine

A

Competes with ACh for its binding site on AChE
Carbamoylates AChE, inactivating it for extended periods of time (increase ACh)

Actions mimic cholinergic stimulation

Does not cross BBB because of charge

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18
Q

Edrophonium

A

Competes with ACh for its binding site on AChE -> ACh

In myasthenia gravis it allows greater # of depleted ACh receptors to bind ACh, results in increase of muscular strength

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19
Q

Echothiophate

A

Phosphorylates AChE -> Increase ACh

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20
Q

Pralidoxime

A

Reactivates AChE by displacing phosphoryl group from AChE that has been inhibited by organophosphates

Give within 24 hours of exposure

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21
Q

Atropine

A

Competitive muscarinic receptor antagonist

Main clinical effects are decreased exocrine gland secretions, mydriasis, cycloplegia, increased HR, decreased tone of bladder/detrusor, decreased tone of GI smooth muscle -> decreased GI motility, bronchodilation

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22
Q

Oxybutynin

A

Competitive muscarinic receptor antagonist

Antimuscarinic effect is less than atropine
Antispasmodic activity is greater than atropine (4-10x great on detrusor muscle)

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23
Q

Ipratropium

A

Muscarinic receptor antagonist, blocks ACh effect on bronchial smooth muscle

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24
Q

Mecamylamine

A

Competitive antagonist at Nn receptor

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25
Q

Epinephrine

A

Mixed-acting agonist, activates both alpha and beta receptors throughout body

In open-angle glaucoma, epinephrine in the eye decreases IOP and produces brief mydriasis

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26
Q

Phenylephrine

A

Selective alpha1 agonist; vasoconstriction

No substantial effect on beta1 receptors of heart or beta2 on bronchi or peripheral blood vessels

Local application causes vasoconstriction of nasal vessels, decreasing mucosal edema to produce decongestant effect

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27
Q

Clonidine

A

Agonist at presynaptic alpha2
Inhibition of sympathetic outflow and tone -> decreased sympathetic tone reduces HR, TPR, MAP, CO, and SV

Hypotensive effect due to actions on brain stem

Epidural produces analgesia that is not blocked by opioid antagonists

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28
Q

Isoproterenol

A

Potent beta 1 and beta 2 agonist
Little or no effect on alpha receptors

Increase in CO ( + inotropic and + chronotropic)
Decrease vascular resistance -> decrease BP and prevents/relieves bronchoconstriction

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29
Q

Dobutamine

A

Primarily beta1 agonist
Minor beta2 and alpha2 effects
R(+) isomer is potent beta1 agonist and alpha1 antagonist
S(-) isomer is weaker mixed beta agonist and alpha1 agonist

Increase myocardial contractility and SV with modest chronotropic effects, increased CO

30
Q

Albuterol

A

Moderately selective beta2 agonist

Stimulates receptors of lung smooth muscle -> relaxation and bronchodilation

Inhibit degranulation and subsequent release of inflammatory substances from mast cells

31
Q

Salmeterol

A

Highly selective beta2 agonist

Stimulates receptors of lung smooth muscle causing relaxation and bronchodilation

32
Q

Phentolamine

A

Competitive antagonist at alpha1 and alpha2 receptors at nanomolar concentrations

Can block 5-HT receptors, K+ channels, and release histamines from mast cells at micromolar concentrations

Inhibition of vasoconstriction -> decrease BP

33
Q

Phenoxybenzamine

A

Noncompetitive, selective alpha1 antagonist (100:1 vs. alpha2), forms stable covalent bond with alpha receptors

Vasodilation, decreased pupillary dilation, lid retraction, inhibition of adrenergically mediated sweating, and reflex tachycardia

34
Q

Prazosin

A

Competitive antagonist at postsynaptic alpha1

Peripheral vasodilation reducing vascular resistance and BP

Relaxes bladder neck and prostate by blocking alpha1 receptors located in smooth muscle, causing less pressure on urethra and leading to increased urine flow

35
Q

Tamsulosin

A

Competitive antagonist at postsynaptic alpha1; 10x selective for alpha1A vs alpha1B (approx. 70% of alpha1 receptors in prostate are alpha1A)

Relaxes bladder neck and prostate by blocking alpha1A causing smooth muscles to relax

36
Q

Yohimbine

A

Antagonist at central presynaptic alpha2 receptors, produces an increase in noradrenergic nerve activity and increase in sympathetic tone

Increases penile blood inflow, decreases penile blood outflow, causes erectile stimulation without increased sexual desire

37
Q

Carvedilol

A

Racemic mixture, both isomers are alpha1 antagonists, S enantiomer is nonselective beta1 and 2 antagonist

Decreases vasoconstriction, decreased BP, increased ejection fraction

Beta1 blockade prevents reflex tachycardia normally associated with alpha1 receptor antagonists and decreases tachycardia associated with sympathetic compensatory mechanisms in HF

38
Q

Propranolol

A

Competitive nonselecive beta-adrenergic receptor antagonist

Decreases resting and exercise HR and CO, decrease systolic and diastolic BP, decrease skeletal muscle perfusion

Beta receptor blockade can decrease somatic symptoms of anxiety such as palpitations and tremor, improvement in psychological components

39
Q

Timolol

A

Competitive nonselective beta adrenergic receptor antagonist

Reduces IOP by reducing aqueous humor production

40
Q

Metoprolol

A

Competitive beta1 selective antagonist

Decrease in resting and exercise HR and CO and decrease in systolic and diastolic BP

41
Q

Pindolol

A

Nonselective beta receptor partial agonist
Attenuates sympathetic tone, does not eliminate it entirely

Decrease in HR, CO, and systolic and diastolic BP

Partial agonist at 5-HT1A, augment anxiolytic effects of SSRIs

42
Q

Alpha-Methyltyrosine

A

Blocks tyrosine hydroxylase (catalyzes first step of catecholamine synthesis)

1-4g QD will reduce catecholamine synthesis 35-80%

Decreased frequency and severity of hypertensive attacks with associated headache, nausea, sweating, tachycardia

43
Q

Alpha-Methyldopa

A

Prodrug, converted in vivo to alpha-methylnorepinephrine (false neurotransmitter)

Major site of action is alpha2 autoreceptors in brainstem -> decrease NE release -> decrease sympathetic tone and decrease baroreceptor response

44
Q

Reserpine

A

Inhibits vesicular neurotransmitter storage, causes long-lasting depletion of 5-HT, NE, and DA in CNS and periphery (decreased neurotransmitter release when neurons depolarize)

Decrease in peripheral vascular resistance and decrease BP, often associated with bradycardia, CO, renal blood flow, and GFR

45
Q

Botulinum Toxin A

A

Specific for cholinergic neurons

Zinc proteinase: cleaves SNAP-25 required for vesicle fusion (decrease ACh release)

46
Q

Amphetamine

A

Indirect-acting sympathomimetic: inhibits NE, DA, and 5-HT uptake transporters
Evokes monoamine release via reverse transport

47
Q

Cocaine

A

Reversibly decreases permeability to Na+, inhibiting electrical conduction

Inhibits neuronal transportation for uptake of 5-HT, E, NE, DA

Produces local vasoconstriction (facilitates examination and surgery by decreasing congestions, swelling, bleeding)
CNS effects are euphoria, stimulation, decreased fatigue, loquacity, sexual stimulation, increased alertness

48
Q

Paroxetine

A

Highest specificity for 5-HT uptake transporters of all SSRIs

Slight anticholinergic activity

49
Q

Atomoxetine

A

NRI, no appreciable 5-HT or DA transporter affinity or affinity for other receptor sites

50
Q

Phenelzine

A

Nonselective, irreversible inhibitor of MAO

Reduction in MAO activity causes an increased concentration of epinephrine, NE, 5-HT, DA

51
Q

Cyclophosphamide

A

Bifunctional alkylating agent; forms DNA-DNA protein cross-links

Prodrug: requires 4-hydroxylation to become cytotoxic

Tissue selectivity (to neutralize toxic intermediate) may result from the capacity of normal tissues to degrade the activated intermediate via aldehyde dehydrogenase, glutathione transferase

CCNS drug

52
Q

Temozolomide

A

Prodrug; spontaneously hydrolyzed and decarboxylated to a monofunctional DNA alkylating agent; inhibits DNA synthesis and function

Methylates DNA mainly at N7 (95%) and O6 of guanine residues (antitumor activity correlates best with 06 methylation)

CCNS drug

53
Q

Carboplatin

A

Enter cells via active Cu++ transporter, CTR1

Oxylate moiety is displaced by water molecules to generate a positively charged and highly reactive molecule that reacts with nucleophilic sites to produce both interstrand and intrastrand DNA cross-links

N7 of guanine is reactive, leads to platinum cross-links between adjacent guanines

CCNS drug

54
Q

Bleomycin

A

Binds to DNA, generates oxygen free radicals (opens deoxyribose ring to create single and double stranded breaks)

CCS drug, causes accumulation of cells in the G2 phase

55
Q

Doxorubicin

A

Intercalates between DNA base pairs (inhibits DNA and RNA polymerase)

Stabilizes DNA-topoisomerase II enzyme complex, inhibits topoisomerase II re-ligation activity, leading to DS DNA breaks and apoptosis

Forms superoxide anion and hydroxyl radicals that damage cell components, stimulated by Fe

CCNS drug

56
Q

5-Fluorouracil

A

Pyrimidine analog, metabolized to fluorodeoxyuridine monophosphate (FdUMP)
FdUMP blocks thymidylate synthase (required for conversion of dUMP –> TMP)
Decreases DNA and RNA synthesis

Produces FdUTP which is incorporated into DNA and RNA

Addition of leucovorin (folic acid derivative) enhances toxicity of 5-FU

CCS drug

57
Q

Gemcitabine

A

Pyrimidine analog, metabolized to mono- di- and tri-phosphate nucleotide analogs that inhibit DNA polymerase
dFdCTP incorporated into DNA to cause strand termination
Inhibits replication and repair synthesis metabolism

Toxicity not confined to S-phase

58
Q

Methotrexate

A

Folic acid analog, high-affinity active site inhibitor of DHFR (dihydrofolate reductase)
Depletion of reduced folates required for dTTP and purine synthesis = decreased DNA, RNA, and protein synthesis

Converted to MTX-polyglutamates which accumulate and inhibit TS and other enzymes

CCS drug

59
Q

Vincristine

A

Binds tubulin, disrupting microtubule assembly and mitotic spindle formation

CCS drug

60
Q

Paclitaxel

A

Promotes polymerization and assembly of microtubules making them extremely stable and nonfunctional

CCS drug

61
Q

Etoposide

A

Forms tertiary complex with DNA and topoisomerase II and stabilizes complex which prevents religation of DS breaks
Cell cycle stops due to DS break accumulation, induces apoptosis

CCS drug (mainly S –> G2)

62
Q

Irinotecan

A

Prodrug, needs cleavage by hepatic carboxylesterases

Stabilizes normally transient DNA-topoisomerase I, leading to accumulation of SS-DNA breaks, collision of DNA replication fork with opened strand and irreversible DS-DNA break

CCS drug, ongoing DNA synthesis is required for cytotoxicity (S-phase specific)

63
Q

Bevacizumab

A

VEGF inhibitor
Binds VEGF-A and prevents it from interacting with target VEGF receptors
Inhibits angiogenesis
Inhibits cell growth, induces apoptosis

CCNS drug

64
Q

Cetuximab

A

Binds extracellular domain of human EGFR to inhibit signaling

Inhibits cell growth, induces apoptosis, induces antibody-dependent cellular toxicity

CCNS drug

65
Q

Rituximab

A

Binds CD20 (B-lymphocyte antigen); expressed >90% of B cells in NHL

Promotes lysis of B-cells by cytotoxic immune cells (antibody-dependent cellular cytotoxicity)

CCNS drug

66
Q

Trastuzumab

A

Binds external HER2/neu tyrosine kinase receptor to prevent activation by EGF; decreases downstream signaling, metastatic potential, promotes apoptosis

Induces antibody-dependent cellular toxicity

CCNS drug

67
Q

Temsirolimus

A

Binds FKBP, complex then binds and inhibits mTOR (kinase involved in upstream regulation of protein synthesis, cell growth, proliferation)

Inhibits G1 –> S

68
Q

Erlotinib

A

Reversible inhibitor of EGFR; binds to ATP binding pocket in receptor tyrosine kinase domain of the EGFR, prevents autophosphorylation of receptor following EGF binding and receptor dimerization

Clinical effect is decrease in cellular growth

69
Q

Imatinib

A

Targets constitutively active BCR-Abl tyrosine kinase receptor created by Philadelphia chromosome 9:22 translocation

Competitive inhibitor of ATP binding domain, prevents binding and hydrolysis of ATP, effectively blocking BCR-Abl and other tyrosine kinase-mediated substrate phosphorylation

Decreases cell growth and proliferation

70
Q

Sunitinib

A

Competitive inhibitor of ATP binding domain, prevents binding and hydrolysis of ATP

Inhibitor of multiple receptor tyrosine kinases including PDGF receptors, VEGF receptors, stem cell factor receptor and others in tumor growth and metastasis

Inhibition of angiogenesis, invasion, metastasis

71
Q

Dantrolene

A

Inhibits the Ca2+ release channel (ryanodine receptor) on the sarcoplasmic reticulum, reducing Ca2+ release

72
Q

Succinylcholine

A

Fast onset; rapid sequence induction/intubation

Short Duration

FM1 (6 decks)

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