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ACVIM General - Imp stuff > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is the MOA of Mycophenolate Mofetil?

A

Humoral -mediated immunity,S-phase(DNA)
* Prodrug of mycophenolicacid(MPA)— needs to be hydrolyzed to be active
* Inhibits inosine monophosphate dehydrogenase (IMPDH)
* IMPDH = enzyme necessary for de novo purine synthesis
* Type2IMPDH(lymphocytes)»Type1(mostcells)
* Inhibits B- and T-cell proliferation and clonal expansion
* Downregulates expression of adhesion molecules

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2
Q

What are the adverse effects of Mycophenolate Mofetil?

A
  • GI (anorexia, vomiting, diarrhea) * (Papillomatosis)
  • (Allergic reactions)
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3
Q

What is the MOA of leflunomide? SE?

A

PYRIMIDINE SYNTHESIS INHIBITOR that inhibits autoimmune T-cell proliferation + AB production of B-cells

  • Reversible inhibition of dihydro-orotate dhydrogenase
    Prodrug that is metabolized by intestinal mucosa and liver to active metabolite (teriflunomide)

SE: GI, eles, hemorhage, leukopenia, thrombocytoenia, anemia, hypercholestelonemia

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4
Q

How is mycophenolate excreted and metabolized?

A

Enterohepatic recirculation – secondary plasma
peak 4-12 hours after oral administration

90% excreted in urine, mostly as MPAG

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5
Q

What are the adverse effects of leflunomide?

A
  • GI (anorexia, vomiting, diarrhea)
  • Spontaneous bleeding
  • Myelosuppression
  • Hepatotoxicosis
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6
Q

What is the MOA of chlorambucil?

A
  • Alkylating agent: cross links DNA
  • Humeral and cell-mediated immunity
  • B cells > T cells
  • Cell-cycle-NON-specific
  • Prodrug
  • Liver→active metabolite (Phenylacetic acid)
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7
Q

What are adverse effects of chlorambucil?

A
  • GI (anorexia, vomiting, diarrhea)
  • Myelosuppression (delayed- 1 month)
  • Alopecia (esp. Poodles)
  • Neurological side-effects in cats
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8
Q

What is the MOA of cyclophosphamide (cytoxan)?

A
  • Alkylating agent:crosslinksDNA
  • Humeral and cell-mediated immunity
  • B cells > T cells * Prodrug
  • Liver→4-hydroxycyclophosphamide + acrolein

Safe for MDR

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9
Q

What are the adverse effects of cyclophosphamide?

A
  • Acrolein→sterile hemorrhagic cystitis - Furosemide might reduce risk
  • GI
  • Alopecia (esp. Poodles)
  • Myelosuppression
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10
Q

What is the MOA of glucocorticoids?

A
  • Humoral and cell-mediated immunity
    Cytoplasmic receptor with DNA sequence binding

(1) ↓ mononuclear phagocytic activity: ↓ Fc receptor expression;
↓ macrophage antigen presentation to TH (immediate)
(2) Elution of antibodies from surface of target cells (immediate)
(3) ↓ inflammatory cell migration into tissues (immediate)
(4) Suppress production of immunoglobulins (delayed)

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11
Q

What are adverse effects of glucocorticoids?

A
  • Iatrogenic hyperadrenocorticism
  • (GI ulceration)
  • Recurrent UTI
  • Pancreatitis
  • Diabetogenic
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12
Q

What is the MOA of cyclosporine?

A

Calcineurin inhibitor
Immunosuppressive that focuses on cell-mediated immunity (T-lymphocytes)

Binds intracellular receptors immunophilins (cytophilin) –> Inhibits calcineurin (phosphatase) blocking dephosphorylation of NFAT (transcription factor)

Inhibits IL-2,Il-3,IL-4,TNF-alpha

Cytochrome P450A - enterocytes and liver
It’s a substrate of P-glycoprotein - enterocytes

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13
Q

What are the side effects of cyclosporine?

A
  • GI (anorexia, vomiting, diarrhea)
  • Gingival hyperplasia
  • Hypertrichosis, hirsutism
  • Papillomatosis
  • (heptatotoxicosis,nephrotoxicity),(lymphoma)
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14
Q

Is cyclosporine to be given with or without food?

A

Food decreases oral absorption (dogs, not cats)

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15
Q

What is the MOA of azathioprine?

A

Thiopurine (purine [adenine, guanine] analog)
Cell-mediated immunity, especially lymphocytes
S-phase (DNA)

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16
Q

What breeds have reduced activity of TPMT? What does this mean?

A
  • REDUCED ACTIVITY: Giant Schnauzers, CATS
    ➔↑ risk of myelosuppression
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17
Q

What breed has increased activity of TPMT?

A

Alaskan Malamutes

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18
Q

Any contraindications between allopurinol and azathioprine?

A
  • Dose reduce if receiving allopurinol (XO inhibitor)
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19
Q

What are the adverse effects of azathioprine?

A
  • GI (anorexia, vomiting, diarrhea)
  • Myelosuppression (leukopenia > anemia,
    thromobytopenia)
  • Hepatotoxicosis (idiosyncratic)
  • Secondary infections
  • Acute pancreatitis
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20
Q

What is the MOA of zolendronate? SE?

A

Inhibit osteoclast mobilization of
bone.

SEs- nephrotoxicity, esophagitis/e-stricture, nausea, diarrhea, hypocalcemia,
hypophosphatemia, hypomagnesemia

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21
Q

What is the MOA of Toceranib (Palladia)? What it is used for? What are the SE?

A

Receptor Tyrosine Kinase Inhibitors
MCT, AGASACA, GIST, Metastatic OSA

SEs- GI ulceration, proteinuria, myelosuppression, GI, muscle and joint pain, hypopigmentation

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22
Q

What is the MOA of Diazoxide (benzoderivative)? What is it used for?

A

MOA. - inhibits insulin secretion from pancreatic B-cells by inhibition of the ATP-dependent K+ channel
Used for insulinomas

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23
Q

What is the MOA of Streptozoon? Uses? SE?

A

MOA: cytotoxic to pancreatic B-cells
SEs- nephrotoxic, diabetes, vomiting
Uses: insulinoma

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24
Q

What is the MOA of ketoconoazole and SE?

A

Ketoconazole- cytochrome P450 inhibitor  inhibits multiple enzymes in the steroid synth. path.
Hepatotoxicity

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25
What are H2 receptor blockers?
famotidine, ranitidine, cimetidine (also inhibits P450)
26
What are H1 receptor blockers?
diphenhydramine, phenothiazines, meclizine, dimenhydrinate
27
What is the MOA of amphotericin B? SE?
macrolide antibiotic that binds to the ergosterol in the cell membrane and alters its permeability --> leakiness and cell death SEs- nephrotoxicity by binding to renal tubular epithelium, acute anaphylaxis
28
What are first tier abx?
-cephalosporins (cefpodoxine, cefocevin) -amoxicillin clauv -clindamycin -potentiated sulfas
29
What are second tier abx?
-doxy, minocycline -chloramphenicol -fluoroquinolones -rifampin - ahminoglycosides
30
What are third tier abx?
-linazolid -vancomycin -teicoplanin
31
MOA of cerenia (maropitant)
Neurokinin-1 receptor antagonist Inhibit binding of substrate P to NK1R in vomiting center, CTZ< GIT Visceral analgesia, anti-inflammatory
32
MOA ondansetron
5HT3 receptor ANTAGONIST Inhibits serotonin-induced stimulation of afferent
33
MOA cisapride
5HT-4 receptor AGONIST - enhances release of Act at myenteric plexus w/o stimulating nicotinic or muscarinic receptor or without inhibiting acetylcholinesterase activity 5HT2alpha receptor AGONIST on colonic smooth muscle 5HT1 + 5HT3 ANTAGONIST of cholinergic neurons
34
MOA erythromycin
Prokinetic, macrolide abx Bacteriostatic, unless high concentrations or Strep Time dependent Macrolines bind 50S ribosomal unit
35
MOA doxycycline
Tetracyclin abx Time dependent, bacteriostatic abx - inhibits protein synthesis by reversibly binding to 30S ribosomal subunit Tetracyclines used for: most Mycoplasma, spirochetes (including Borrelia burgdorferi, Lepto, Chlamydia, Anaplasma, Ehrlichia, Rickettsia), some Mycobacterium spa Some gram positive activity
36
What defect is found in herding breeds that cautions to use certain medications?
4-bp deletion in the ABCB1 gene (previously MDR1 gene)
37
What chemotherapeutics are not safe for dogs. with ABCB1 gene depletion?
Doxorubicin Mitoxantrone Vincristine Vinblastine Paclitaxel and docetaxel
38
What is the MOA of slentrol?
Not on the market anymore Dirlotapide - triglyceride transfer protein inhibitor --> blocks trig uptake into enterocytes an causes satiety
39
MOA and SE ifosfamide
Antineoplastic Alkylating agent chemical reactivity is nonspecific - alkylation of cancer cell DNA strains SE: neutropenia, damage to urinary bladder epithelium, nephrotoxic (primarily on prox and distal tubules), GI signs, neurotoxic, alopecia, ELEs
40
MOA of clopidogrel
ADP receptor (PY2) binds irreversibly
41
Chemo drug that cases arrest in M-phase
Vincristine, vinblastine, Paclitaxel and docetaxel
42
Chemo drug that effects S-phase
Cytosar, Gemcitabine, 5-FU
43
Alkylating chemo drugs
Chlorambucil Melphalan Cycloposphamide Lomustine Dacarbazine Streptozotocin
44
platinum chemo drugs
Cisplatin, carboplatin
45
MOA and SE diazoxide
Direct vasodilator/hyperglycemic Activates K channels Used to tx insulinomas - most common SE hyper salivation, V, D, tachycardia SE: hematologic abnormalities (agranulocytosis, aplastic anemia, thrombocytopenia), pancreatic, DM, cataracts, Na/H2o retention
46
MOA and SE oclacitinib
Apoquel JAK kinase ibhibitor Antipruritic, anti-inflammatory SE (most common): diarrhea, vomiting, anorexia
47
MOA and SE amphotericin B
Antifungal Binds to sterols (primarily ergosterol) in fungal cell membrane SE: nephrotoxic (renal vasoconstriction reduces GFR Lipid complex and liposomal - more hydrophobic so reduces nephrotoxic qualities-- mediates uptake in reticuloendothelial cells in liver and decreases dose to kidneys
48
MOA pimobendan
Ca2+ sensitizer (via PDEi3i) Vasodilator
49
MOA TMS
Potentiated sulfonamide antimicrobial -- inhibit enzymes in folic acid pathway --> inhibit bacterial thymine synthesis Bacteriostatic - sulfonamides Bactericial - trimethoprim Spectrum -Gram positive (Nocardia, most streptococci, staphylococci) -Gran neg (Enterobacteriaceae) -Good penetration to PROSTATE Inefective against: Pseudomonas, protozoa (Pneumocystis, Coccidia, Neospora, Toxo) SE: KCS, acute neutrophilic hepatitis w icterus, V, D, fever, hemolytic anemia, urticaria, facial swelling, PUPD, cholestasis -Clinical hypothyroidism -Acute hypersensitivity -- type I (anaphylaxis), type III (formation of antigen:ab complex) - more common in large dogs (Doberman, Samoyeds, mini schnauzer)
50
MOA and SE enrofloxacin
Fluoroquinolone Inhibit bacterial topoisomerase II (DNA gyrase) + topoisomerase IV --> prevent DNA supercoil and synthesis Bactericidal and concentration dependent SE: GI, rarely ELEs, ataxia, seizures Cats: ocular toxicity (mydriasis, retinal degeneration, blindness) - cats have AA changes in ABCG2 transporter in BBB Articular cartilage abnormalities in young, growing animals
51
MOA and SE propantheline
Quaternary antimuscarinis -antispasmodic/antisecretorry effects of diarrhea Use: AV block, detrusor hyperreflexia or urge incontinence MOA: antimuscarinic (similar to atropine) -does not cross BBB SE (similar to atropine): dry mouth an eyes, urinary hesitancy, tachycardia, constipation -V, hypersalivation cats
52
Drug to use for inflammatory brain disease
Cytosar -affects S-phase SE: myelosupppression, decreased PLT
53
MOA and SE calcitriol
Vitamin D analog Bind yo vite receptors to decrease PTH
54
How do we tx Babesia Gibson?
Atovaquone and azithromycin
55
MOA and SE Atovaquone
Oral antiprotozoal agent With azithro - also good for tx cats w/Cytauxzoon MOA: targets protozoan mitochondrial electron transport SE: vomiting
56
What is the tx for Pneumocystosis in dogs
First line: Potentiated sulfonamides Second line: Atovaquone
57
MOA and SE of azithromycin
Macrolide abx Bacteriostatic MOA: Inhibit protein synthesis of 50S ribosomal subunits in bacteria Use: tx of bacteria, rickettsial, protozoal info, reduce gingival hyperplasia caused by cyclosporine, canine papillomatosis SE: GI
58
How to tx Cytaux
Atovaquone and azithromycin
59
What drug do we give a pheochromocytoma? MOA? SE?
Phenoxybenzamine MOA: non-selective alpha adrenergic antagonist, vasodilador -- chemical sympathomimetic No effects on beta or PNS SE: associated with alpha blockade (hypotension, weak, dizzy, GI, meiosis, increased IOP, Na retention, tachycardia
60
What drug is the primary to use ion USMI? MOA? SE?
Phenylpropanolamine (Proin) MOA: non-selective alpha AGONIST -sympathomimetic - indirectly stimulates alpha and to less extent beta (release of NE) Side effects: hypertension, restlessness/anxiety, tachycardia, increased IOP, hepatic glycogenolysis
61
MOA L-asparagonase?
-enzyme derived from E. colia dn wrinia carotovora MOA: catalyzes asoaraginase into ammonia + aspartic acid SE: *Hypersensitivity after repeated uses -hypersensitivity reactions (including anaphylaxis) -elevated liver enzymes (reversible) -hypercoagulability with thrombous formation -pancreatitis (dogs only) -myelosuppression (less common), moreso when combined with vincristine
62
How to tx tritrichomonas? SE/MOA?
Ronidazole MOA: 5-niitroimidazole - converted by hydrogenosome into polar autootix anion radicals SE (similar to metro): tremors, ataxia, seizure, neurotoxicity
63
What medication to give during acetaminophen toxicity? SE?
Silymarin (milk thistle) - liver protectant SE: V, anorexia, itching
64
Tx for copper toxicity?
D-penicillamine MOA: chelating agent (Cu, Fe, mercury) SE: -anorexia, vomiting, diarrhea – frequent! (giving with food can decrease this) -teratogen -long term effects: anemia (normocytic or microcytic) and glycogen storage of liver, glomerulonephritis, proteinuria
65
MOA and SE trilostane?
MOA: competitive inhibitor of 3-B-hydroxysteroid dehydrogenase SE: electrolyte derangements (hypoNa, hyperK, , V, D, A
66
MOA/SE PENICILLINS?
MOA: -Inhibit penicillin binding proteins (PBP) – enzymes involved in building bacterial cell wall -Only active against rapidly multiplying organisms -Gram negative lipopolysaccharide decreases antibiotic penetration -Time dependent -Bactericidal -low VD
67
MOA of panoquell
Leukocyte function-associated antigen 1 (LFA-1) antagonist
68

ACVIM General - Imp stuff (11 decks)

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