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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
Epinephrine
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
26
Phenylephrine
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
27
Clonidine
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
28
Isoproterenol
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
29
Dobutamine
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
Albuterol
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
Salmeterol
Highly selective beta2 agonist Stimulates receptors of lung smooth muscle causing relaxation and bronchodilation
32
Phentolamine
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
Phenoxybenzamine
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
Prazosin
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
Tamsulosin
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
Yohimbine
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
Carvedilol
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
Propranolol
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
Timolol
Competitive nonselective beta adrenergic receptor antagonist Reduces IOP by reducing aqueous humor production
40
Metoprolol
Competitive beta1 selective antagonist Decrease in resting and exercise HR and CO and decrease in systolic and diastolic BP
41
Pindolol
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
Alpha-Methyltyrosine
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
Alpha-Methyldopa
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
Reserpine
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
Botulinum Toxin A
Specific for cholinergic neurons Zinc proteinase: cleaves SNAP-25 required for vesicle fusion (decrease ACh release)
46
Amphetamine
Indirect-acting sympathomimetic: inhibits NE, DA, and 5-HT uptake transporters Evokes monoamine release via reverse transport
47
Cocaine
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
Paroxetine
Highest specificity for 5-HT uptake transporters of all SSRIs Slight anticholinergic activity
49
Atomoxetine
NRI, no appreciable 5-HT or DA transporter affinity or affinity for other receptor sites
50
Phenelzine
Nonselective, irreversible inhibitor of MAO Reduction in MAO activity causes an increased concentration of epinephrine, NE, 5-HT, DA
51
Cyclophosphamide
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
Temozolomide
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
Carboplatin
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
Bleomycin
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
Doxorubicin
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
5-Fluorouracil
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
Gemcitabine
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
Methotrexate
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
Vincristine
Binds tubulin, disrupting microtubule assembly and mitotic spindle formation CCS drug
60
Paclitaxel
Promotes polymerization and assembly of microtubules making them extremely stable and nonfunctional CCS drug
61
Etoposide
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
Irinotecan
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
Bevacizumab
VEGF inhibitor Binds VEGF-A and prevents it from interacting with target VEGF receptors Inhibits angiogenesis Inhibits cell growth, induces apoptosis CCNS drug
64
Cetuximab
Binds extracellular domain of human EGFR to inhibit signaling Inhibits cell growth, induces apoptosis, induces antibody-dependent cellular toxicity CCNS drug
65
Rituximab
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
Trastuzumab
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
Temsirolimus
Binds FKBP, complex then binds and inhibits mTOR (kinase involved in upstream regulation of protein synthesis, cell growth, proliferation) Inhibits G1 --> S
68
Erlotinib
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
Imatinib
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
Sunitinib
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
Dantrolene
Inhibits the Ca2+ release channel (ryanodine receptor) on the sarcoplasmic reticulum, reducing Ca2+ release
72
Succinylcholine
Fast onset; rapid sequence induction/intubation Short Duration

FM1 (6 decks)

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