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MOA Reboot > MOA > Flashcards

MOA Flashcards

1
Q

Cabergoline

A

Dopamine agonist

Decreases prolactin

Causes luteolysis and decreases progesterone

Can stop lactation

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2
Q

PGF2a

A

Luteolytic - causes decline in progesterone

Causes uterine contractions

Opens cervix and increases glandular secretions

(Do not give if cervix is closed)

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3
Q

Oxytocin

A

Peptide hormone released by posterior pituitary

Mobilizes intracellular Ca and causes influx of Ca. (Gs GPCR)

Alters transmembrane ion currents and increases Na permeability of myometrium

Causes sustained uterine contractions

Also stimulates milk ejection and is involved in luteolysis

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4
Q

Pentoxyphylline

A

Non-selective PDE inhibitor

Increases RBC deformability, reduces blood viscosity, decreases potential for PLT aggregation and clot formation

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5
Q

Diphenhydramine

A

H1 receptor antagonist

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6
Q

Diazoxide

A

Hyperglycemic: Inhibits insulin secretion(by opening K ATP channels which lets K leave, hyperpolarizes cell, no Ca entry which inhibits insulin), stimulates hepatic gluconeogenesis and glycogenolysis, stimulates epinephrine release, inhibits tissue use of glucose

Also has direct vasodilator effect on peripheral arterioles

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7
Q

Allopurinol

A

Xanthine oxidase inhibitor

Used for acute tumor lysis syndrome (XO converts purines to uric acid)

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8
Q

Vinca Alkaloids

A

Vincristine, vinblastine, vinorelbine

Binds to tubulin and prevents formation of mitotic spindle

Causes metaphase arrest

Vincristine can cause peripheral neuropathies

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9
Q

Alkylating Agents

A

Cyclophosphamide, chlorambucil, lomustine(CCNU), melphalan

Bind alkyl groups to DNA creating cross links

Inhibits DNA uncoiling and replication

Toxicity: alopecia, BM,GI. Cyclophosphamide causes sterile hemorrhagic cystitis

Chlorambucil causes neurotoxicity, hepatotox with CCNU

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10
Q

Platinum Agents

A

Cisplatin, carboplatinum

Bind platinum groups to DNA creating cross links

Inhibits DNA uncoiling and replication

cortical blindness (cisplatin), nephrotoxic in dogs (cisplat), fatal pulmonary edema in cats (cisplat)

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11
Q

Anthracycline Antibiotics

A

Doxorubicin, mitoxantrone

Multiple MOAs, halts cell division and stimulates apoptosis

Topoisomerase II inhibition

DNA intercalation

Generation of free radicals

Doxo causes DCM after 6 doses, hemorrhagic colitis

Extravasation is bad (give dexrazoxane)

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12
Q

L-asparaginase

A

Converts asparagine to aspartate and ammonia - depletes asparagine

Normal cells can synthesize asparagine but LSA cells lack asparagine synthetase

Without asparagine, protein synthesis is halted

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13
Q

Antimetabolites

A

5-FU, cytosar (cytosine arabinoside), methotrexate, hydroxyurea

Analogues of normal cell metabolism compounds or nucleic acid bases

Inhibit use of cell metabolites in growth and division

Incorporated into DNA or RNA to prevent replication

5-FU cases fatal neurotoxicity in cats.

hydroxyurea specifically inhibits DNA synthesis by blocking the action of ribonucleoside diphosphate reductase

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14
Q

Palladia (toceranib)

A

Tyrosine kinase inhibitor

Can cause PLN in dogs, nephrotoxicity in cats

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15
Q

Metoclopramide

A

D2 antagonist: antiemetic. (central so has extrapyramidal effects)

5-HT4 agonist: prokinetic

5-HT3 antagonist: antiemetic (peripheral)

increases LES tone

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16
Q

Domperidone

A

D2 antagonist. peripheral and central? antiemetic in CRTZ and increases ACh release in GI tract to promotes motility. but doesnt cross BBB…

Alpha 2 and beta 2 antagonism to GIT

minimal effects on LES

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17
Q

Cisapride

A

Parasympathomimetic

5-HT4 and 5-HT2 agonist: prokinetic

5-HT3 and 5-HT1 antagonist

does not cross BBB so no extrapyramidal effects. increases LES tone.

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18
Q

Ondansetron

A

5HT3 antagonist
Anti-emetic

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19
Q

Erythromycin/Azythromycin
(for prokinetic effects)

A

Motilin receptor agonist

may decrease LES tone

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20
Q

Ranitidine

A

H2 receptor antagonist (suppresses gastric acid)

Inhibits acetylcholinesterase in GIT (stimulates motility)

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21
Q

Omeprazole

A

Protein pump inhibitor

Decreases gastric acid production by inhibiting H+/K+ ATPase in parietal cells

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22
Q

Famotidine

A

H2 receptor antagonist

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23
Q

Maropitant

A

NK1 receptor antagonist

Inhibits binding of substance P

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24
Q

Misoprostol

A

PGE1 analog

decreases cAMP

Inhibits gastric acid secretion

Increases gastric mucus and bicarbonate

Increases turnover of mucosal cells and enhances mucosal blood flow

enhances tight junctions among epithelial cells

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25
Q

Prochlorperazine/Chlorpromazine

A

Anti-emetic

Dopamine antagonist

H1 antagonist

Alpha 2 antagonist

Muscarinic antagonist. also 5Ht2 antag.

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26
Q

Sucralfate

A

Negatively charged sucrose sulfate binds to positively charged proteins in the base of ulcers or erosion, forms a physical barrier that restricts further caustic damage

Inhibits back diffusion of H+ ions, inactivates pepsin, absorbs bile acids

Stimulates mucosal prostaglandin and bicarbonate secretion

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27
Q

Penicillamine

A

Chelates copper, lead, iron, and mercury

Anti-fibrotic (inhibits collagen cross linking)

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28
Q

Colchicine

A

Anti-fibrotic: stimulates collagenase activity

Inhibits cell division by interfering with mitotic spindle

Inhibits synthesis and secretion of serum amyloid A

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29
Q

Urosdiol

A

Increases bile flow by increasing expression of membrane transporters

Suppresses absorption, synthesis, and secretion of cholesterol

Immunomodulatory (decreases NFkB, IL-1, and IL-2)

Protects hepatocytes from bile acids

Stabilizes mitochondria to prevent apoptosis and increases glutathione

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30
Q

S-Adenosyl-Methionine (SAMe)

A

Glutathione precursor

Essential part of:

Transmethylation (methyl donor)

Transsulfuration

Aminopropylation (thiol donor)

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31
Q

Silymarin, Silibinin (Milk Thistle)

A

Free radical scavenger

Inhibits lipid peroxidation and beta-glucuronidase

Reduces hepatic collagen formation and increases glutathione content

Inhibits cytotoxic effects of TNF

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32
Q

N-acetylcysteine

A

Glutathione precursor

Thiol donor

Sulfur donor

Free radical scavenger

(NOT a methyl donor like SAMe)

Improves hepatic blood flow via increased NO production

Mucolytic: reduces disulfide bonds in mucoproteins

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33
Q

Vitamin E

A

Antioxidant

Prevents action of peroxidase on cell membranes

(Competes with Vit K - do not use in coagulopathic patients)

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34
Q

Lactulose

A

Nonabsorbable disaccharide that gets digested to volatile FA and reduces colonic pH

Converts NH3 to NH4+ which gets trapped in the gut and excreted

Inhibits colonic bacterial production of ammonia and increases ammonia incorporation into colonic bacteria

Osmotic agent - increases colonic transit speed

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35
Q

L-Ornithine L-aspartate (LOLA)

A

L-ornithine is substrate of urea cycle

L-aspartate is substrate in conversion of NH3 to glutamine

May be beneficial in ammonia detox pathways

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36
Q

Cholestyramine

A

Binds to bile acids in GIT to prevent enterohepatic recycling

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37
Q

Benzodiazepines

A

Midazolam, Diazepam

Binds to GABA receptor and increases its affinity for GABA

Results in increased Cl influx and hyperpolarization of the postsynaptic cell membrane

Other possible mechanisms: antagonism of serotonin, increased release of GABA, and diminished release or turnover of Ach in the CNS

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38
Q

Phenobarbital

A

Barbiturate

Interacts with GABA receptor and prolongs opening of Cl channels resulting in hyperpolarization of the neuron

Also inhibits glutamate receptors and voltage-gated Ca channels. SE: hepatotoxicity, blood dyscrasia (immune mediated), superficial necrolytic dermatitis

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39
Q

Potassium Bromide

A

Causes hyperpolarization of the neuron via movement of bromide ions intracellularly through chloride channels

Can cause fatal pneumonitis in cats; pancreatitis in dogs

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40
Q

Zonisamide

A

Sulfonamide drug with multiple MOAs

Inhibition of voltage-gated Na channels

Inhibition of T-type Ca channels

Modulation of dopaminergic activity

Enhancement of GABA activity in the CNS

Inhibition of carbonic anhydrase activity

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41
Q

Levetiracetam

A

Binds to synaptic vesicle protein SV2A which results in decreased neurotransmitter release

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42
Q

Propofol

A

Potentiates effects of GABA

Decreases the rate of dissociation of GABA from its receptors

May also potentiate activity at glycine receptor and antagonize activity at NMDA receptors. Hepatic metab mostly except cats where lungs help out (although can induce oxidative heinz body anemia in cats). Reduces ICP and CMRO2 but also CePP.

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43
Q

Inhalant Anesthetics

A

Gaba-A agonist (maybe?)

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44
Q

Mannitol

A

Osmotic diuretic

Rheologic mechanism most important for reduction in ICP (immediate)

-Draws water out of other body tissues much more readily than brain

-Results in immediate plasma expansion and decreased blood viscosity -> decreased cerebral vascular resistance and transient increase in CBF

-Cerebral vasoconstriction causes CBF to return to normal

-Total cerebral blood volume is decreased leading to decreased ICP while maintaining CBF

Osmotic effect to reduce brain water is delayed 15-30 minutes

Also has free radical scavenging properties.

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45
Q

Gabapentin and Pregabalin

A

Bind to alpha-2-delta subunit of neuronal voltage-gated Ca channels and reduces Ca influx into neurons

Leads to inhibition of release of excitatory neurotransmitters

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46
Q

Baclofen

A

GABA-B agonist

Opens K channels and hyperpolarizes cells —> inhibits release of excitatory neurotransmitters in the spinal cord

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47
Q

General Opioid MOA

A

Opioid receptor is Gi protein

Binding results in inhibition of AC and reduced cAMP in cells

Also interacts with ion channels producing an activation of K conductance (post synap) and inhibition of Ca conductance (presynapt)

Net effects: reduced intracellular cAMP, hyperpolarization of cell, reduced neurotransmitter release.

Also inhibit GI transit by reducting ACh release via M2R centrally and peripherally

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48
Q

Butorphanol

A

Opioid agonist-antagonist

Kappa agonist

Mu antagonist

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49
Q

Buprenorphine

A

Opioid - partial mu agonist

Very high affinity for mu receptor but only produces partial response

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50
Q

Methadone

A

Opioid - full mu agonist

Presynaptically: closes Ca channels - reduced NT release

Postsynaptically: opens K channels - hyperpolarization

NMDA antagonist

Reduces reuptake of norepinephrine

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51
Q

Fentanyl

A

Opioid - full mu agonist

Short acting

80-100x more potent than morphine

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52
Q

Tramadol

A

Opioid - mu receptor agonist

Inhibits reuptake of norepinephrine and serotonin

NMDA antagonist

In humans, analgesia is dependent on metabolism to the M1 metabolite (O-demethyltramadol) but this does not occur in dogs. Does occur in cats

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53
Q

Etomidate

A

GABA-A agonist

Increases Cl conductance leading to hyperpolarization

Cardiovascularly sparing

Decreases ICP (if high) while maintaining CPP

Can cause adrenocortical suppression

Hyperosmolar - can cause hemolysis

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54
Q

Alfaxalone

A

GABA-A agonist

At low concentrations, modulates ion currents through GABA receptor

At high concentrations, direct GABA agonist

Dose dependent respiratory depression; also CV depression, but generally insignificant at clinical doses. decreases ICP and CBF and CMRO2

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55
Q

Flumazenil

A

Competitive antagonist of benzodiazepines at benzodiazepine receptors on GABA-A receptor

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56
Q

Ketamine

A

Dissociative anesthetic

Non-competitive NMDA antagonist - prevents glutamate from binding

Causes dissociation of the limbic and thalamocortical systems

Also acts at mu, delta, and kappa opioid receptors

Acts at monoaminergic receptors (antinociception)

Antagonistic activity at muscarinic receptors (anticholinergic effects)

Increases sympathetic tone and inhibits reuptake of norepinephrine

Increases ICP, negative inotropic effect. decreases BP but with more norepi, usually fine, unless patients exhausted catecholamine stores (eg critical illness).

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57
Q

Amantadine

A

NMDA antagonist

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58
Q

Atropine

A

Anticholinergic (parasymp antagonist)

Competitively antagonizes Ach at postganglionic muscarinic cholinergic receptors in PNS

Effects on heart mediated by pre and postsynaptic M2 receptors in SA and AV nodes and atrial myocardium —> increase in sinus rate, acceleration of AV nodal conduction, increased atrial contractility

Paradoxical worsening of bradycardia after administration due to more rapid blockade of presynaptic M1 receptors which inhibits negative feedback. Causes transient increase in Ach release and slowing of heart rate

Bronchodilation and reduced airway secretions via M2 and M3

Ophtho: Mydriasis, relaxes pupillary sphincter muscle

decreased tear production, decreased saliva production, ileus

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59
Q

Glycopyrrolate

A

Anticholinergic

Competitively antagonizes Ach at postganglionic muscarinic cholinergic receptors in PNS

4x more potent than atropine, slower onset of action, longer duration

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60
Q

Dantrolene

A

Ryanodine receptor antagonist

Peripherally acting muscle relaxant

Reduces Ca release from SR

Used for malignant hyperthermia and rhabdomyolysis

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61
Q

Methocarbamol

A

Centrally acting muscle relaxant

Selectively inhibits spinal and supraspinal polysynaptic reflexes through its interactions with interneurons

No direct effects on skeletal muscle

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62
Q

Succincylcholine

A

Depolarizing NMBA

Binds to and activate nicotinic receptor

Not susceptible to acetylcholinesterase

Ion channel remains open and repolarization does not occur

Initial uncoordinated muscle contractions and then flaccid paralysis. Can see Hyperkalemia (bc Na/Ca/K channels open for a long time - especially problematic in chronic injuries where there are many extrajunctional ACh R), increased ICP/IOP/intragastric pressure, muscle soreness

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63
Q

Pancuronium

A

Non-depolarizing NMBA

Also blocks cardiac muscarinic receptors —> tachycardia

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64
Q

Atracurium, Cisatracurium

A

Non-depolarizing NMBA; short-acting

Binds to but does not activate postsynaptic nicotinic receptor at NMJ

Degraded by Hofmann elimination and ester hydrolysis

Decomposes to laudanosine, a CNS stimulant that can cause seizures

Can cause histamine release

Can occasionally act on muscarinic or nicotinic receptors in ANS causing cardiovascular effects (tachycardia)

Cisatracurium is 4x as potent as atracurium (lower doses = less laudanosine = lower chance of CNS effects); less potential for histamine release

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65
Q

Vecuronium, Rocuronium

A

Non-depolarizing NMBAs

No cardiovascular effects

No histamine release

Rocuronium has faster onset of action, but less potent than vecuronium

Hepatic metabolism, bile and renal clearance

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66
Q

Edrophonium

A

Acetylcholinesterase inhibitor

Reversible inhibition

Brief duration of action

Not specific for NMJ - can see muscarinic signs (bradycardia, bronchospasm, meiosis, ileus, salivation) - treat with atropine or glycopyrrolate

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67
Q

Neostigmine, Pyridostigmine

A

Acetylcholinesterase inhibitors

Irreversible binding

Prevents breakdown of Ach (not specific for NMJ; can cause muscarinic signs)

Neostigmine works faster, pyridostigmine lasts longer

68
Q

Local Anesthetics

A

Lidocaine, proparacaine, bupivacaine, mepivacaine

Inhibit Na channels and decrease AP propagation

Also inhibit K and Ca channels at level of spinal cord - may contribute to antinociception by blocking sensory pathways

Also inhibit tachykinins (e.g. substance P) and glutamate transmission leading to less depolarization of NMDA and NK receptors

69
Q

Dexmedetomidine

A

Alpha 2 agonist

Presynaptic activation of alpha 2 receptor inhibits NE release

Postsynaptic activation inhibits sympathetic activity

Activation of inwardly rectifying K channels results in hyperpolarization and decreases firing rate of excitable CNS cells

Reduces Ca conductance into cells, inhibiting NT release; involves direct action on N-type voltage gated Ca channels (independent of cAMP)

Locus coeruleus has highest density of alpha 2 receptors; important for vigilance and nociceptive neurotransmission

Also works on alpha 2 receptors in spinal cord

70
Q

Apomorphine

A

D2 receptor agonist in CRTZ

71
Q

Acepromazine

A

Phenothiazine tranquilizer

Block postsynaptic dopamine receptors in CNS

Alpha-1 antagonist

72
Q

Methimazole

A

Inhibits thyroid peroxidase

73
Q

Potassium Iodide

A

Used for treatment of thyroid storm.

Oral potassium iodide prevents peripheral conversion of T4 to T3

Have to give AFTER methimazole.

Also inhibits formation/release of the hormone

74
Q

Octreotide

A

Somatostatin analogue

Inhibits synthesis and secretion of insulin, glucagon, secretin, GH, gastrin, and motilin

Canine insulinoma cells have a high affinity for octreotide

75
Q

Trilostane

A

Inhibitor of 3-beta hydroxysteroid dehydrogenase

Reduces synthesis of cortisol, aldosterone, and adrenal androgens

Inhibition is reversible and dose-dependent

76
Q

Mitotane

A

Causes selective adrenal necrosis of zona fasciculata and reticularis

Spares zona glomerulosa (although not entirely true)

Also inhibits several enzymes required for steroid synthesis

77
Q

Selegiline

A

MAO-type B inhibitor

Normally MAO-B is responsible for reuptake of dopamine

Dopamine causes suppression of ACTH

Used to treat pituitary dependent Cushing’s

78
Q

Desoxycorticosterone Pivalate (DOCP)

A

Long-acting mineralocorticoid

No glucocorticoid action

79
Q

Fludricortisone

A

Synthetic corticosteroid

High mineralocorticoid and moderate glucocorticoid activity

Addisonian patients often still need to take prednisone since would not get enough corticosteroid activity

80
Q

Short Acting Insulins

A

Regular

Lispro

Aspart

Glulisine

81
Q

Intermediate Acting Insulins

A

NPH (Humulin N, Novolin N)

Vetsulin/Lente

Prozinc/PZI

82
Q

Long Acting Insulins

A

Glargine/Lantus

Detemir/Levemir

Tesiba/Degludec

83
Q

Doxapram

A

Respiratory stimulant

Activates peripheral chemoreceptors within carotid bodies

At high doses, stimulates medullary respiratory center

84
Q

Theophylline

A

Methylxanthine

PDE III (and IV) inhibitor —> increased levels of cAMP

Smooth muscle dilation in bronchi and pulmonary vasculature

Can cause central respiratory stimulation

Stimulates diaphragmatic contractility and prevents fatigue

85
Q

Aminophylline

A

Methylxanthine

PDE III (and IV) inhibitor —> increased levels of cAMP

Smooth muscle dilation in bronchi and pulmonary vasculature

Can cause central respiratory stimulation

Stimulates diaphragmatic contractility and prevents fatigue

86
Q

Rutin

A

Stimulates macrophage breakdown of protein in lymph, enhancing its reabsorption

Used for chylothorax

87
Q

Beta-lactam antibiotics

A

Penicillins, cephalosporins, carbapenems

Inhibit peptidoglycan synthesis thus inhibiting cell wall synthesis

Bactericidal

Time-dependent

Generally good for gram +, gram -, and anaerobes

88
Q

Fluoroquinolones

A

Enrofloxacin, marbofloxacin, ciprofloxacin, pradofloxacin

Inhibits DNA gyrase and topoisomerase IV - prevents uncoiling and separation of DNA strands —> inhibits DNA replication

Bactericidal

Concentration dependent

Good for gram -, limited gram + (staph), bad for anaerobes, works well for intracellular organisms (mycoplasma)

89
Q

Aminoglycosides

A

Amikacin, gentamicin, streptomycin, tobramycin

Inhibits protein synthesis by inhibiting 30S ribosomal subunit

Bactericidal

Concentration dependent

Great for gram -, some gram +, no anaerobes

90
Q

Chloramphenicol

A

Inhibits protein synthesis by inhibiting 50S ribosomal subunit

Mostly bacteriostatic (can be cidal at higher concentrations)

Time dependent

Broad spectrum (gram +, gram -, anaerobes; does not get pseudomonas)

91
Q

Clindamycin

A

Lincosamide

Inhibits protein synthesis by inhibiting 50S ribosomal subunit

Bacteriostatic or cidal depending on concentration

Time dependent, concentration enhanced

Best for gram + and anaerobes, toxo/neospora, some mycoplasma

92
Q

Erythromycin, Azithromycin (ABX MOA)

A

Macrolides

Inhibits protein synthesis via 50S ribosomal subunit

Mostly bacteriostatic (can be cidal at high conc)

Azithro=Concentration dependent
Erythro=Time dependent, concentration enhanced.

Best for gram + and anaerobes, some mycoplasma-azithrosomegramnegtoo

93
Q

Trimethoprim/Sulfamethoxazole

A

Potentiated sulfonamide

Interferes with folic acid synthesis by preventing addition of PABA into folic acid molecule; folic acid needed for synthesis of nucleic acid

Bactericidal

Time or concentration dependent (depending on pathogen)

Gram + and many gram -, some protozoa, not good for anaerobes

94
Q

Metronidazole

A

Causes strand breaks in DNA - results in inhibition of protein synthesis and cell death

Bactericidal

Concentration dependent

Anaerobes and protozoa

95
Q

Tetracyclines

A

Inhibits protein synthesis by inhibiting 30S ribosomal subunit

Bacteriostatic (may be cidal at high concentrations)

Time-dependent, concentration enhanced

Wide range of gram +, gram -, anaerobes, and atypical organisms (mycoplasma, chlamydiae, rickettsiae, protozoa)

96
Q

Vancomycin

A

Glycopeptide

Binds to peptide precursors in cell wall and inhibits cell wall synthesis

Also affects bacterial RNA synthesis

Bactericidal (static for enterococci)

Time dependent

Gram + aer and anaer

97
Q

Amphotericin B

A

Macrocyclic polyene antibiotic (antifungal medication)

Binds to ergosterol in cell membrane and increases membrane permeability (forms micelles with hydrophilic core, inserts into fungal cell membrane and creates transmembrane ion channel)

Usually fungicidal, has postfungal effect

Very broad spectrum (all common systemic mycoses)

Nephrotoxicity

98
Q

Azole Antifungals

A

Inhibit lanosterol 14-alpha demethylase, a P450 enzyme responsible for ergosterol synthesis

Imidazoles (ketoconazole, miconazole, clotrimazole)

Triazoles (fluconazole, itraconazole, voriconazole, posaconazole)

May also inhibit mammalian P450 enzymes

Generally first line for most systemic mycoses (except cryptococcus)

(Usually itraconazole, unless CNS or ocular involvement, then fluconazole)

99
Q

Mycophenolate

A

Inhibits purine synthesis by inhibiting inosine monophosphate dehydrogenase –>
Inhibits T/B cells and suppresses B cell formation of antibodies

SE: GI, ulcerative colitis

100
Q

Cyclosporine

A

Binds to cyclophilin and inhibits calcineurin dependent T cell activation.

Blocks release of IL2 and IFNg from T helpers

SE: severe GI upset, gingival hyperplasia

101
Q

Azathioprine

A

Antagonizes purine synthesis so inhibits proliferation of T and B cells.

SE: mild GI, hepatotox, myelosuppression

102
Q

Leflunomide

A

Pyrimidine synthesis inhibitor so prevents DNA/RNA synth.

Inhibits T cell proliferation and autoantibody production by B cells

SE: elevated LES, myelosuppresion

103
Q

Epinephrine

A

Alpha 1, alpha 2, beta 1, and beta 2 agonist (+++)

contract: +++

HR +++

CO ++

tone +++

BP +++

104
Q

Norepinephrine

A

+++ alpha 1 and alpha 2

+ beta 1

contract: +

HR: variable

CO: variable

tone +++

BP +++

105
Q

Dopamine

A

Endogenous precursor to norepinephrine

Also causes release of NE from sympathetic nerve terminals

Low dose (1-4 mcg/kg/min) = dopaminergic - inhibition of NE release, splanchnic vasodilation

Medium dose (5-10 mcg/kg/min) = beta 1 (++) and beta 2 (+) - increased contractility and HR

High dose (10-20 mcg/kg/min) = alpha 1 and alpha 2 (++) - increased SVR

Table results:

contract ++

HR ++

CO variable

Tone ++

BP ++

106
Q

Dobutamine

A

Beta 1 agonist (++)

Also some beta 2 (+) and alpha 1 (+)

Contract ++

HR +

CO ++

tone -

BP variable

SE: Tachycardia, Arrhthymias, GI

107
Q

Phenylephrine

A

Alpha 1 and 2 agonist (+++) —> increased SVR

No beta

contract: 0

HR: -

CO: -

tone: +++

BP: +++

108
Q

Vasopressin

A

V1 (vascular smooth muscle): vasoconstriction (Gq pathway)-IP3 acts on IP3 sensitive Ca channel on the ER → release of Ca, forms Ca-calmodulin complex that activates the MLCK and with ATP, phosph MLC → vasoconstriction. DAG stays in the cell and stimulates the influx of Ca through a Ca channel which acts with CM but also on a JAK2 pathway to prevent smooth muscle relaxation by inhibiting MLCphosphatase. also acts on the K ATP sensitive channel, closing them so get depolarized and Ca can enter.

—causes NO release in some vascular beds (cerebral, renal, mesenteric, pulm) —> dilation

–also platelets have V1 –> increased Ca and thrombosis

–also kidneys –> reduced blood flow to inner medulla, contraction of efferent arteriole to increased GFR

V2 (kidney): Gs –> increased cAMP. AQP2 inserted in distal nephron, water resorption

– also stimulates release of plt from bone marrow and release of vWBF and F8 from endothelial cells

V3 (anterior pituitary): release of ACTH. Gq. also some insulin effects

TABLE:

contractility: 0

HR/CO: -

tone/BP: ++

109
Q

Desmopressin (DDAVP)

A

Stimulates V2 receptors —> insertion of AQP2 channels —> water resorption

Causes release of vWF from endothelial cells and macrophages

Less vasopressor (V1) activity than arginine vasopressin

110
Q

Ephedrine

A

Sympathomimetic amine

Alpha (+) and beta 1+2 agonist (+) and increases release of NE from sympathetic nerve endings

contract: +

HR: +

CO: +

tone: variable

BP: +

Bronchodilation

111
Q

Nitroprusside

A

Oxidizes sulfhydrl groups in RBCs and cell membranes or reacts with Hb to produce metHb - these reactions produce NO (as well as 5 cyanide groups)

Causes vasodilation, reducing BP and afterload dilates arteries and veins, arteries more

NO–>cGMP → inhibition of Ca influx into smooth muscles → decreased Ca/calmod stimulation of MLCK → decreased contraction.

Can cause cyanide toxicity

SE: hypotension, nausea

112
Q

Nitroglycerin

A

Converted to NO

Relaxes vascular smooth muscle, primarily of venous side

Leads to decreased preload

Also can have dose dependent reduction in afterload

SE: hypotension, syncope/headache

113
Q

Isoproterenol

A

Beta 1 and 2 agonist (+++).

vasodilator, may augment forward flow but caution with BP

contract: +++

HR: +++

CO: +++

tone: - - -

BP: - - -

114
Q

Amlodipine

A

Calcium channel blocker with preference for vascular smooth muscle (dihydropyridine)

Inhibits L-type Ca channel

Causes vasodilation

afferent art > efferent so can cause decreased GFR

SE: hypotension, lethargy, gingival hyperplasia

115
Q

Nicardipine

A

Calcium channel blocker with preference for vascular smooth muscle (dihydropyridine)

Inhibits L-type Ca channel

Causes vasodilation

afferent art > efferent so can cause decreased GFR

SE: hypotension, nausea, weakness

116
Q

Hydralazine

A

Direct arterial vasodilator

SSAO inhibitor - alters cellular Ca metabolism in smooth muscle. prevents oxidation of NO and inhibits IP3 induced Ca release from the SR.

SE: hypotension, weakness, leth

117
Q

Phenoxybenzamine

A

Non-selective alpha antagonist

Relaxes internal urethral sphincter and lowers SVR (alpha 1)

Inhibition of presynaptic alpha 2 receptors results in more NE release - counteracts SVR effects of alpha 1 blockade.

takes a week to kick in.

118
Q

Prazosin

A

Alpha 1 antagonist

relaxes the internal urethral sphincter - reduces pre and prostatic pressure but not post prostatic intraurethral pressure or penile urethra so questionable in UOs. SVR decreases with minimal effects on CO

119
Q

Bethanechol

A

Parasympathomimetic

Directly stimulates muscarinic receptors

In bladder leads to contraction of detrusor muscle and expulsion of urine

Used to treat urinary retention, dysautonomia, and incontinence

120
Q

Phenylpropanolamine

A

PPA, Proin

Partial alpha-1 agonist

Causes release of NE and inhibits its reuptake at synaptic junction

Causes increases urethral sphincter tone

121
Q

Furosemide

A

-Inhibits Na-K-2Cl cotransporter in thick ascending limb of the loop of Henle

-When inhaled, acts at pulmonary venodilator and bronchodilator, relieves dyspnea

-mostly it is secreted by OAT in prox tubule so acidemia may prevent secretion of lasix

-Causes vasodilation and decreased peripheral vascular resistance, Lowers preload by diuresis and venodilation

-“Renal protective” - Reduces renal tubular O2 demand by preventing NA absorption

-Chronic administration →distal tubule hypertrophy and upreg of NKCC

-Adverse effects: hypoNa, hypoK, hypoCl, hypoMg, metabolic alk, hypotension and hypovolemia, ototoxicity, mucosal dehydration in trachea, panc, interferences with thyroid testing

122
Q

Thiazides

A

Inhibits Na/Cl cotransporter in early DCT —> decreased Na reabsorption —> diuresis

In nephrogenic DI causes a decrease in UOP:

-Inhibits Na/Cl transport in early DCT and prevents dilution of urine in this segment - results in Na loss and ECF contraction and decreased GFR

-Over time this volume contraction leads to increased Na and water reabsorption in PCT —> less filtrate presented to distal nephron so less excreted as urine

SE: GI upset, Hypokalemia Hypochloremic alkalosis Hyponatremia Hypomagnesemia Hypercalcemia

123
Q

Spironolactone

A

Potassium sparing diuretic

Aldosterone antagonist

-in principal cells of DCT/CD: Less ENaC, less ROMK, , less activity of Na/K ATPase

-in alpha intercalated cells of CD, less activity of H-ATPase

overall increased Na, Ca,and H2O excretion, less K+/H+ excretion

SE: GI disturbances, facial dermatitis in cats

124
Q

Fenoldapam

A

D1 agonist

Produces more renal vasodilation and natriuresis than dopamine

Causes systemic hypotension (but maintains GFR)

125
Q

Clopidogrel

A

Platelet Inhibitor

Binds to P2Y12 receptor on PLT membrane and inhibits ADP binding

Inhibits PLT activation, granule secretion, integrin activation, and thromboxane A2 production

Irreversible

126
Q

Aspirin

A

COX-1 inhibitor (and a little COX2)

Reduces prostaglandin and thromboxane A2 synthesis

TXA2 is a PLT agonist

Platelets unable to synthesize their own new COX

127
Q

Abciximab

A

Anti-platelet drug

GP IIb/IIIa receptor (alpha-IIb-beta-3) inhibitor

128
Q

Ticagrelor

A

Anti-platelet drug

P2Y12 receptor inhibitor (reversible)

129
Q

Warfarin

A

Vitamin K antagonist

Inhibits Vit K epoxide reductase therefore inhibiting the recycling of Vit K

Vit K normally carboxylates factors II, VII, IX, and X (activates them). vit K also needed for protein C and S so little bit of procoag activity.

130
Q

Unfractionated Heparin

A

Binds and potentiates AT: inhibits FIXa, FXa, FXIa, FXIIa, and FIIa (thrombin)

Most profound inhibitory effects on thrombin and FXa (1:1 ratio)

Also causes release of TFPI from endothelial surface (so direct anticoagulant)

(Inhibits activation of FXIII —> prevents formation of stable fibrin clot??)

Highly protein bound, less predictable bioavailability

131
Q

Low Molecular Weight Heparin

A

eg dalteparin/enoxaparin.

Binds and potentiates AT

Binds FIIa and FXa —> preferentially inhibits FXa (more 4:1 for X:II)

Not big enough to bind both AT & thrombin (so less inhibition of thrombin)

Since most activity against FXa, little effect on aPTT at standard doses - anti10a levels best

Bioavailability more predictable bc less protein bound

Longer half-life

132
Q

Rivaroxaban

A

Factor Xa inhibitor

133
Q

Tranexamic acid, Aminocaproic acid

A

-Synthetic lysine analogues

-Bind to plasminogen (at fibrin’s lysine binding site) and prevent conversion to plasmin

-Inhibits plasmin directly at higher doses

-TXA 10x more potent than ACA and longer half life

134
Q

Streptokinase

A

Nonspecific plasminogen activator

Combines with plasminogen to form complex that converts plasminogen to plasmin (binds both circulating and fibrin-bound plasminogen)

Plasmin degrades fibrin, fibrinogen, plasminogen, coag factors, and streptokinase

135
Q

Urokinase

A

Plasminogen activator

Binds with increased affinity to the lysine-plasminogen form (as opposed to the glutamate) which differentially accumulates within thrombi - fibrin-specific

136
Q

Tissue Plasminogen Activator (tPA)

A

Primary activator of plasminogen in vivo

Does not readily bind circulating plasminogen - does not induce a systemic proteolytic state at physiologic levels

Has high affinity for fibrin in thrombi- results in relatively fibrin-specific conversion of plasminogen to plasmin.

At recommended high clinical doses, a systemic proteolytic state and bleeding can occur

137
Q

Procainamide (also quinidine)

A

Class 1A antiarrhythmic - inhibits fast Na channels (moderate)

Moderate reduction in slope of phase 0 and amplitude of AP

Decreases conduction velocity in non-nodal tissue

Also inhibits K delayed rectifiers: prolongs effective refractory period and action potential duration

Also has some anitcholinergic effects (mild)

indications: monomorphic VT mostly, also Afib, atrial flutter, SVTs

SE: bradycardia, hypotension

138
Q

Lidocaine

A

Class 1B antiarrhythmic - inhibits fast Na channels (weak)

Mild reduction in slope of phase 0 and amplitude of AP

Decreases conduction velocity in non-nodal tissue

Decreases effective refractory period and action potential duration

Local anesthetic: inhibits Na channels and decreases AP propagation

Systemic analgesic mechanisms not well understood, likely many including action at ion channels (Na, Ca, K) and NMDA receptors

Inhibits ROS formation and lipid peroxidation

enhanced activity with tachycardia, acidosis, hyperkalemia, and ischemic/diseased tissue

SE: GI/seizures

139
Q

Mexiletine

A

Class 1B antiarrhythmic - inhibits fast Na channels (weak)

Mild reduction in slope of phase 0 and amplitude of AP

Decreases conduction velocity in non-nodal tissue

Decreases effective refractory period and action potential duration

indication: ventric arrhytm

SE: nausea, vomiting, ataxia

140
Q

Flecainide, Propafenone

A

Class 1C Antiarrhythmics

Inhibit fast Na channels (strong)

Large reduction in slope of phase 0 and amplitude of AP

Decreases conduction velocity in non-nodal tissue

No change in effective refractory period or action potential duration

indication: ventric arrhythm, SVT, A-fib

SE: arrhythmias (ventricular tachycardia - induces moreso than other agents in this class),

141
Q

Propranolol

A

Beta blocker, non-selective (Class II antiarrhythmic)

Inhibits funny current (Na) and L-type Ca channels.

Decreases sinus rate and contractility, depresses conduction through AV node (specifically, by blocking B1, prevents phosphorylation of L-type Ca channels and phospholamban so SERCA inhibited)

Decreases myocardial oxygen demand

Can inhibit conversion of T4 to T3 (useful in thyroid storm)

High first-pass effect (IV dosages ~10% of oral dose)

indications: SVT (not as good as CCB), inappropriate sinus tach (slows SA), V-tach secondary to increased symp tone. beta agonist toxicity, thyroid storm.

Dont give with SA dysfn (block/arrest), AV node conduction disturbance, pulm dz, CHF, systolic dysfn

SE: bradycardia, bronchoconstriction

142
Q

Atenolol/Esmolol

A

same as propranolol

Beta-blocker, beta-1 selective (Class II antiarrhythmic)

Decreased sinus rate, slowed AV conduction

Decreases myocardial oxygen demand

esmolol super short acting.

esmolol: SVT –> SE RTA, metabolic acidosis

atenolol: SVT, pulm stenosis –> SE fatigue

143
Q

Sotalol

A

Class III antiarrhythmic - K channel blocker

Blocks K channels responsible for phase 3 repolarization

Causes increase in action potential duration and effective refractory period so predisposes to early after depolarization

Increases Q-T interval

works best at low HR

used for SV and ventricular arrhythmias esp ARVC

Also has class II activity (beta-blocker, nonselective)

144
Q

Amiodarone

A

Class III antiarrhythmic - K channel blocker

Blocks K channels responsible for phase 3 repolarization

Causes increase in action potential duration and effective refractory period

Increases Q-T interval

Also has properties of Class I, II, and IV - less arrhythmogenic than sotalol and decreased early after depolarization risk

indications:Unstable V-tach, A fib, V fib.

SE: interstitial lung disease/hypersensitivity pneumonitis, peripheral neuropathy

145
Q

Diltiazem

A

Class IV antiarrhythmic - Ca channel blocker

Blocks L-type Ca channels

Nondihydropyridine - acts primarily on nodal cells

Slows AV node conduction, prolongs rise and repolarization of AP, and prolongs effective refractory period, prolongs PR interval. may speed myocardial relaxation and dilate coronary arteries so improve diastolic fn by improving coronary perfusion

-slows ventric rate to atrial tachyarrhythmias and prolongs AV node so tachyarrhythmia can be terminated

indication: SVT (including a-fib, a flutter)

SE: hypotension, bradycardia, GI signs

146
Q

Verapamil

A

Class IV antiarrhythmic - Ca channel blocker

Blocks L-type Ca channels

Nondihydropyridine - acts primarily on nodal cells

Slows AV node conduction, prolongs effective refractory period, prolongs PR interval, negative inotrope

147
Q

Digoxin

A

Inhibits Na/K ATPase

Leads to increased intracellular Na —> inhibits Na/Ca exchanger —> less Ca pumped out of cells —> increased intracellular [Ca] —> positive inotropy

Also increases vagal tone to heart —> reduction in SA firing rate (decreased HR) and decreased conduction velocity through AV node

Hypokalemia can cause digoxin toxicity because K competes with digoxin for binding

indication: afib

SE: Arrhythmias, GI, CNS

148
Q

Pimobendan

A

PDE3 inhibitor, inodilator

Sensitizes troponin C to calcium —> increased contractility

also PDE3 inhibition —> increased cAMP—> more pKA, and thus: (1) phosphorylation of phospholamban –> more SERCA reuptake of Ca++, (2) more phosphorylation of L-type Ca channels –> more Ca entry –> increased contractility. also get veno/arterial vasodilation.

Does NOT increase intracellular Ca concentration

SE: GI upset, may cause arrhythmias

149
Q

Sildenafil

A

PDE5 inhibitor

Inhibits the breakdown of cGMP in pulmonary vasculature

Increased cGMP results in NO mediated vasodilation in pulmonary vasculature

150
Q

Enalapril

A

ACE Inhibitor

Prevents conversion of Ang I to Ang II —> reduced aldosterone release, reduced peripheral vasoconstriction, reduced plasma volume.

also causes an increase in bradykinin → arterial and venous vasodilation.

151
Q

Benazepril

A

ACE Inhibitor

Prevents conversion of Ang I to Ang II —> reduced aldosterone release, reduced peripheral vasoconstriction, reduced plasma volume

also causes an increase in bradykinin → arterial and venous vasodilation.

152
Q

Telmisartan

A

Angiotensin II Receptor Blocker

Reduces aldosterone release, peripheral vasodilation (arterial and venous), and decreases plasma volume via excretion of Na

SE: GI upset, hypotension

153
Q

Algepristone

A

Progesterone receptor antagonist

Converts closed to open cervix

Results in expulsion of material w/in 24hours

Not available in US

154
Q

Latanoprost

A

Synthetic PG analog

increased aqueous outflow via uveoscleral outflow, causes miosis to allow more outflow of the normal iridocorneal angle

Do not use if anterior lens lux

Can cause uveitis

155
Q

Dorzolamide

A

Carbonic anhydrase inhibitor

Decreases production of aqueous humor

156
Q

Phenylephrine (ophtho)

A

Sympathomimetic

Selectively binds alpha 1 receptors leading to vessel constriction (hence why we use for hyphema)

157
Q

Tacrolimus

A

inhibits both T-lymphocyte signal transduction and IL-2 transcription

158
Q

Tropicamide

A

parasympathetic antagonist, allows sympathetic actions to dominate

acts on the pupillary sphincter muscle to cause its relaxation and thus dilation

Short acting

159
Q

Hypertonic saline

A

-hyperosmotic resuscitation fluid. allows us to use a smaller volume of fluid to achieve a similar increase in pressure by drawing volume from their interstitial space rather than adding additional intravascular volume (3-4x increase in blood volume compared to the volume administered).

-may help reduce any cerebral edema

-improves CBF by dehydrating cerebrovascular endothelial cells and increasing vessel diameter

-decreases brain excitotoxicty by promoting reuptake of glutamate into intracellular space, and reducing adhesion of PMN cells to microvasculature, modulating the inflammatory response.

improves the rheology of circulating blood

-may have positive effects on myocardial function.

-Caution with hyponatremic patients. Can also aggravate pulmonary edema/contusions because of rapid volume expansion

-May be superior to mannitol in reducing (and sustaining it) ICP and improving CCP

160
Q

Prednisone

A

-decreases phagocytosis of RBC (in IMHA)

-inhibits complement

-decreases cytokines (esp proinflam production via inhibition of NFkB)

-decrease circulating level of T-lymphs

-down regs expression of Fc receptors on macs

161
Q

Mirtazapine

A

TCA that blocks presynaptic A2R, which blocks the normal feedback loop and results in increased norepi.

Also antagonizes: 5HT2, 5HT3, H1.

Can cause agitation, orthostatic hypotension in ppl, hyperactivity, mydriasis.

162
Q

Capromorelin

A

Ghrelin R agonist, stimulates GH release and therefore IGF1 release.

SE: V/D, hypersalivation, nausea, hypotension

163
Q

Cyproheptadine

A

serotonin R antagonist (5Ht2) and H1 R antagonist

appetite stimulant

may cause vocalization, aggression. also inhibits feline airways smooth muscle contraction

164
Q

Terbutaline

A

beta-2 adrenergic receptor agonist

increases cAMP in bronchioles –> activating protein kinase A, inactivation of myosin light-chain kinase, activation of myosin light-chain phosphatase, and relaxing smooth muscle in the bronchiole.

may increase mucociliary clearance and decreased release of inflam mediators from mast cells

165
Q

Milrinone

A

PDE3 inhibitor - prevents cAMP breakdown

↑ cAMP - ↑Ca++

↑ contractility

↑ CO

↑ SV

↑ Heart rate

↑ Ejection fraction

↓ preload & ↓ afterload

PDE3-i: cardiac inotropy, lusitropy, and peripheral vasodilatation

indication:CHF

SE: Ventricular arrhythmias Bronchospasm Hypokalemia

166
Q

hIVIG

A

-binds Fc R on mononuclear cells preventing destruction of plts by inhibiting phagocytosis

-binds pathogenic AutoAB

-decreases cytokine release

-inhibits C3/C4 of complement

-inhibits Fas-Fas binding so get less apoptosis

SE: Anaphylaxis, fever, risk of thromboembolic events (increases conc of circulating thrombin/antithrombin complexes, possibly increases plt activation/number), renal failure, hypotension, fluid overload

MOA Reboot (3 decks)

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