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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
Q

What are H2 receptor blockers?

A

famotidine, ranitidine, cimetidine (also inhibits P450)

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26
Q

What are H1 receptor blockers?

A

diphenhydramine, phenothiazines, meclizine, dimenhydrinate

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27
Q

What is the MOA of amphotericin B? SE?

A

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

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28
Q

What are first tier abx?

A

-cephalosporins (cefpodoxine, cefocevin)
-amoxicillin clauv
-clindamycin
-potentiated sulfas

29
Q

What are second tier abx?

A

-doxy, minocycline
-chloramphenicol
-fluoroquinolones
-rifampin
- ahminoglycosides

30
Q

What are third tier abx?

A

-linazolid
-vancomycin
-teicoplanin

31
Q

MOA of cerenia (maropitant)

A

Neurokinin-1 receptor antagonist
Inhibit binding of substrate P to NK1R in vomiting center, CTZ< GIT
Visceral analgesia, anti-inflammatory

32
Q

MOA ondansetron

A

5HT3 receptor ANTAGONIST
Inhibits serotonin-induced stimulation of afferent

33
Q

MOA cisapride

A

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
Q

MOA erythromycin

A

Prokinetic, macrolide abx
Bacteriostatic, unless high concentrations or Strep
Time dependent

Macrolines bind 50S ribosomal unit

35
Q

MOA doxycycline

A

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
Q

What defect is found in herding breeds that cautions to use certain medications?

A

4-bp deletion in the ABCB1 gene (previously MDR1 gene)

37
Q

What chemotherapeutics are not safe for dogs. with ABCB1 gene depletion?

A

Doxorubicin
Mitoxantrone
Vincristine
Vinblastine
Paclitaxel and docetaxel

38
Q

What is the MOA of slentrol?

A

Not on the market anymore
Dirlotapide - triglyceride transfer protein inhibitor –> blocks trig uptake into enterocytes an causes satiety

39
Q

MOA and SE ifosfamide

A

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
Q

MOA of clopidogrel

A

ADP receptor (PY2) binds irreversibly

41
Q

Chemo drug that cases arrest in M-phase

A

Vincristine, vinblastine, Paclitaxel and docetaxel

42
Q

Chemo drug that effects S-phase

A

Cytosar, Gemcitabine, 5-FU

43
Q

Alkylating chemo drugs

A

Chlorambucil
Melphalan
Cycloposphamide
Lomustine
Dacarbazine
Streptozotocin

44
Q

platinum chemo drugs

A

Cisplatin, carboplatin

45
Q

MOA and SE diazoxide

A

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
Q

MOA and SE oclacitinib

A

Apoquel
JAK kinase ibhibitor
Antipruritic, anti-inflammatory

SE (most common): diarrhea, vomiting, anorexia

47
Q

MOA and SE amphotericin B

A

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
Q

MOA pimobendan

A

Ca2+ sensitizer (via PDEi3i)
Vasodilator

49
Q

MOA TMS

A

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
Q

MOA and SE enrofloxacin

A

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
Q

MOA and SE propantheline

A

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
Q

Drug to use for inflammatory brain disease

A

Cytosar -affects S-phase
SE: myelosupppression, decreased PLT

53
Q

MOA and SE calcitriol

A

Vitamin D analog
Bind yo vite receptors to decrease PTH

54
Q

How do we tx Babesia Gibson?

A

Atovaquone and azithromycin

55
Q

MOA and SE Atovaquone

A

Oral antiprotozoal agent
With azithro - also good for tx cats w/Cytauxzoon

MOA: targets protozoan mitochondrial electron transport

SE: vomiting

56
Q

What is the tx for Pneumocystosis in dogs

A

First line: Potentiated sulfonamides
Second line: Atovaquone

57
Q

MOA and SE of azithromycin

A

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
Q

How to tx Cytaux

A

Atovaquone and azithromycin

59
Q

What drug do we give a pheochromocytoma? MOA? SE?

A

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
Q

What drug is the primary to use ion USMI? MOA? SE?

A

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
Q

MOA L-asparagonase?

A

-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
Q

How to tx tritrichomonas? SE/MOA?

A

Ronidazole
MOA: 5-niitroimidazole - converted by hydrogenosome into polar autootix anion radicals

SE (similar to metro): tremors, ataxia, seizure, neurotoxicity

63
Q

What medication to give during acetaminophen toxicity? SE?

A

Silymarin (milk thistle) - liver protectant

SE: V, anorexia, itching

64
Q

Tx for copper toxicity?

A

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
Q

MOA and SE trilostane?

A

MOA: competitive inhibitor of 3-B-hydroxysteroid dehydrogenase

SE: electrolyte derangements (hypoNa, hyperK, , V, D, A

66
Q

MOA/SE PENICILLINS?

A

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
Q

MOA of panoquell

A

Leukocyte function-associated antigen 1 (LFA-1) antagonist

68
Q
A

ACVIM General - Imp stuff (11 decks)

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