Exam 2 Flashcards by Chelsea curry

o	Little COX1 to 2 selectivity 
o	Equine (sometimes still used in dogs)
o	Good analgesic, antipyretic 
o	NOT intended for food animals

Phenylbutazone

How well did you know this?

Not at all

Perfectly

o No COX1:2 selectivity
o Most broadly used NSAID in LA
• Approved in Eq, Bov
o Treatment duration limited by toxicity (<5 days)

Fluxin meglumine

How well did you know this?

Not at all

Perfectly

o No COX 1:2 selectivity (in clinical use, despite research that shows COX 2 selc)
o Approved in K9
o AVOID feline
o Most frequent problems are GI, renal, hepatic

Carprofen

How well did you know this?

Not at all

Perfectly

o No COX 1:2 selectivity
o Approved in Equine
o Main probs: GI (K9), GI/renal in horses

Ketoprofen

How well did you know this?

Not at all

Perfectly

o COXIB class and highly selective for COX2 enzyme
o Approved for K9
o Has sulfonamide group therefore watch for sulfonamide sensitive animals
o Well tolerated, but still has inclination for side effects, esp. with chronic use

Deracoxib/Dermaxx

How well did you know this?

Not at all

Perfectly

o	New class of dual acting agents that inhibit both COX1 and 2 AND 5-lipoxygenase (LOX)
•	Inhibits formation of PGEs, Txs, LT
o	All actions occur at clinical doses unlike Ketoprofen

Tepoxalin

How well did you know this?

Not at all

Perfectly

Fungistatic
Treatment of dermatophytoses
hepatic microsomal enzyme metabolism
Binds to fungal intracellular microtubules and inhibits mitosis
Renal excretion
GI issues, myelosupressive, teratoenic, skeletal malformations, neutropenia in FIV cats

Griseofulvin

How well did you know this?

Not at all

Perfectly

Do not use this anti-fungal when pt is on Phenobarb, Pheno decreases absorption

Griseofulvin

How well did you know this?

Not at all

Perfectly

Binds to membrane sterols/ergosterol (fungal PM)→permeability changes and leakage of cell contents→cell death
Fungistatic or fungicidal,depending on dose
highly protein bound and metabolized locally at tissue sites
tx of systemic mycoses
Main adverse effect: Nephrotoxicity due to vasoconstriction or direct toxic effect on renal tissues
Used short term due to resistance

Amphotericin B

How well did you know this?

Not at all

Perfectly

o Fungistatic/fungicidal
o MOA: Impairs conversion of lanosterol to cholesterol and ergosterol
• Affinity for fungal, but not 100%
Needs acidic environment because it is water insoluble
(lipophilic)
hepatic metabolism
Various adverse effects: common in cats, GI, hepatotoxicity, pruritis and alopecia and lightening of coat
Caution in geratrics
Broad anti-fungal

Ketoconazole

How well did you know this?

Not at all

Perfectly

Compared to ketoconazole=better absorption, longer duration of action, less toxic, more potent!
MOA: inhibition of ergosterol synthesis = high affinity for fungal enzyme

Trazoles: Fluconazole, Itraconazole

How well did you know this?

Not at all

Perfectly

o high spercificty for fungal cP450 enzyme	
Fewer adverse reactions 
o	Usually well tolerated in cats
o	Broad spectrum 
keratinophilic
Lipophilic
^^ PO absorption

Itraconazole

How well did you know this?

Not at all

Perfectly

o Broad spectrum (just not deep mycoses, does do systemic)
o Safest
o MOA: high specificity for fungal enzyme (cP450)
o Pharacokinetics
• Low protein binding so crosses the BBB and blood CSF barrier
• NO hepatic metabolism
• Renal excretion

Fluconazole

How well did you know this?

Not at all

Perfectly

•	Inhibits squalene epoxidase preventing it from proceeding to ergosterol →cell death
•	NOT a cP450 type enzyme 
Fungicidal
^^ lipophilic 
keratinophilic 
well tolerated

Terbinafine

How well did you know this?

Not at all

Perfectly

chemotherapeutic drugs that work on specific phase of the cell cycle; not effective on cells NOT dividing

phase specific

How well did you know this?

Not at all

Perfectly

chemo drugs that work on a generalized cell cycle; majority of the drugs

phase nonspecific

How well did you know this?

Not at all

Perfectly

•	Hepatic activation, “prodrug”
Phase non-specific 
•	Renal excretion (reduce dose with renal failure)
•	Toxicity 
•	Myelosuppression 
•	GI
•	Sterile hemorrhagic cystitis, Bladder toxicity is the major adverse effect
Used for many tumor types

Cyclophosphamide (alkylating agent)

How well did you know this?

Not at all

Perfectly

• Renal excretion
• Most common uses: Sub for Cyclophosphamide, Chronic lymphocytic leukemia, Feline GI (small cell lymphoma)
• Does NOT cause bladder toxicity issues
Phase non specific

Chlorabucil

How well did you know this?

Not at all

Perfectly

• Completely absorbed after PO (per OS) intake: 1st pass hepatic degradation to active metabolites
• Highly lipid soluble and low MW= cross BBB
• Renal excretion, partial hepatic excretion=enterohepatic cycle
• LOPP protocol
• Toxicity: Myelosuppression, Possible irreversible hepatic toxicity, Neutropenia nadir variable
Phase non specific

Lomustine (in class he said just know it exists and it is hepatotoxic)

How well did you know this?

Not at all

Perfectly

Phase non-specific

Platinum Synthetic Drugs: Will cross BBB and commonly causes nausea

Procarbazine, Cysplatin, Carboplatin

How well did you know this?

Not at all

Perfectly

• LOPP/MOPP rescue protocol
• Myelosuppression
Platinum synthetic drug, phase non-specific

Procarbazine

How well did you know this?

Not at all

Perfectly

Highly protein bound
Renal excretion
Toxicity: Nephrotoxic (give diuretics), Nausea (can treat with antimetics), FATAL pulmonary edema in felines
Primary use: osteosarc, SSC

Cysplatin

How well did you know this?

Not at all

Perfectly

•	Renal excretion 
•	Toxicity: 
o	Myelosuppression
o	Monitor platelets
•	SAFE for felines 
•	Fewer GI side effects of the platinum drugs

Carboplatin

How well did you know this?

Not at all

Perfectly

Cell cycle specific drugs that target the S phase

Purine and/or pyrimidine analogues are inserted into DNA→non-functional DNA

Antimetabolites: Methotrexate, Cystosine arachinoside

How well did you know this?

Not at all

Perfectly

``` • Hepatic metabolism • Renal excretion (Tubular secretion) • Crosses the BBB • Toxicity: GI, Myelosuppression, Reversible by reducing folate drug • Usage: lymphoma, CNS tumors, osteosarc Targets S phase ```

Methotraxate

* Rapid hepatic metabolism * Efficient renal removal from circulation * Ideally given by continuous infusion * Crosses the BBB * Usage: more for neuro tumors

cystosine arachinoside | antimetabolite

Cell cycle specific and cause free radical damage and inhibition of topoisomerase II (prevents DNA from unwinding for transcription)

antibiotics: doxorubicin, mitoxantrone, dactomycin

• Hepatic metabolism (Dose reduction if bilirubin is >2mg/dl) • Renal excretion (Primary route in the cat and May turn urine orange-red) • Toxicity: Anaphylaxis (direct degranulation of mast cells when given), Vesicant (do NOT give outside vein), Cardiotoxicity (dose-dependent) Used for a variety of tumors

Doxorubicin (antibiotic)

* Doxorubicin alternative * Very expensive * Cause myelosuppression

Mitoxanthrone (antibiotic)

``` o Binds DNA at transcription initiation complex and prevents elongation of RNA chain by RNA polymerase • Does NOT cross BBB • Excretion: urine, feces • Non-cardiotoxic sub for Doxorubicin • Used for lymphoma rescue too • Toxicity: myelosuppression, GI ```

Dactomycine aka Actinomycin D (antibiotic)

o Targets M phase • Binds to microtubules of the mitotic spindle o NO class cross resistance Some prevent assembly, some prevent dissembly

Plant alkaloids | Vincristine, Vin blastine, vinorelbine

3 chemo drugs that we need to know that prevent assembly of microtubules of the mitotic spindle (during M phase)

Vincristine, vinblatine, vinerelbine

• Hepatic (biliary) excretion (dose reduction when bili is >2mg/dl) • Toxicity: Vesicant , Myelosuppression , Peripheral neuropathy ο Primary use: lymphoma, transmissible venereal tumor, thrombocytopenia Targets M phase

Vincristine ( plant alkaloid)

* Hepatic (biliary) excretion: dose reduction when bili is >2mg/dl * Toxicity: Vesicant , More myelosuppression than vincristine * Primary use: mast cell tumors, can be used as a sub for vincristine

Vinblastine (plant alkaloid that targets M phase)

* Bind to cytoplasmic receptors and inhibit DNA synthesis * Lympholitic * Toxicity: PU/PD, polyphagia, panting, GI ulceration * Usage: wide range

Prednisone

``` Cell cycle non-specific (max activity in G1 phase though) Toxicity: analphyaxis, potentate vincristine (induced myelosuppression) Alone does NOT cause myelosuppression Primary use: lymphoma ```

L-asparaginase (note: enzyme)

Targeted therapy drugs that are only through a specialist | Main problem is that resistance occurs

Tocerabib, Masitinib (receptor kinase inhibitors)

alkylating agents, antibiotics, platinum drugs are examples of...

cell nonspecific

taxanes, vinca alkaloids, antimetabolites are examples of..

cell specific

Osmotic diuretic, freely filtered at the glomerulus Site: All segments, but mostly the thin descending limb Decreases Na, Cl, K Decrease Ca, P, Mg Impairs passive water reabsorption Not reabsorbed and not metabolized by the body

Mannitol

``` Loop Diruretic Site: Thick ascending limb Decrease Na, K, Cl Decrease Ca, P, Mg Strongest of all groups! ```

Furosemide

``` Thiazide diuretic Block Na-Cl symporters Site: distal tubule Decrease Na, K, Cl Decrease Ca, P, Mg ```

Hydrochlorothiazide

``` Aldosterone antagonist Site: Distal tubule and CD Decrease: Na and Cl Increase: K Decrease Ca ```

Spironolactone (the only one that works from the vascular side)

Carbonic anhydrase inhibitors Site: proximal tubule Decrease Na, K, Cl Decrease P

Acetazolamide

Indicated in cases of cerebral edema and increased intracranial pressure Contraindicated in CHF Maybe renal protective, increases the amount of urine kidneys produce, but not really tx the kidneys

Mannitol

Inhibit Na-K-2Cl symport on luminal side of the thick ascending limb Main use: pulmonary edema due to CHF Increase K, Ca, and Mg excretion Also, increases renal vasodilation (good for kidneys), increases renin secretion (bad for kidneys), increases venous capacitance

Furosemide, strongest diuretic

o Used in combination with a loop diuretic to treat refractory heart failure o Increase renal excretion of K and Mg o Reduce Ca and urate excretion o Not effective at low glomerular filtration rates

Hydrochlorothiazide

o Effect on endothelium of BV and cells that line heart channels o Not used in the treatment of acute CHF o Used in cases of primary hyperaldosteronism or cirrhosis o Poor diuretic o Diminishes the degree of K+ loss, “K sparing diuretic” o Indication: K sparing diuretic

Spirinolactone

• Converts water and CO2→carbonic acid which it is broken down to bicarb and H+, regulates pH • When blocked, decrease in H+ secretion into the urine→more H+ accumulates in body→acidosis weak diuretic Mainly used for glaucoma

Acetazolamide

``` Not controlled Not FDA approved needs low chloride (low salt diet), high diets will increase renal excretion creates a pseudohyperchloremia Toxic in cats Loading doses if used alone ```

Potassium bromide

* Synthesis occurs in mast cells and basophils, ECL (enterochromatin like cells, special cells of the GI tract) cells and CNS * Metabolized in the liver * Major mediator of inflammation, anaphylaxis and gastric acid secretion * Neurotransmitter

Histamine

Venule/arteriole dilation, venoconstriction Bronchoconstriction, increased secretion, mucosal edema Itch and pain Produced tachycardia

H1 receptor

Produce increased acid secretion and ulceration occurs

H2 receptor

medullary (brainstem) stimulant respiratory stimulant ONLY used to stimulate laryngeal function and respiration during a laryngeal examination

doxapram

The more lipophilic and neutral of the H1 antihistamines

First generation (can cross BBB)

o Major uses: allergy, itching, nausea, motion sickness, and insomnia o Limited roles in asthma or anaphylaxis (no role!) o Diphenhydramine

H1 antihistamines

``` Most widely used across species little mineralocorticoid activity Group C/long acting rapid onset potent concern with colonic perforation and laminitis in the horse ```

Dexamethazone

* 1st generation * Serotonin (5-HTP) antagonist * Appetite stimulant * Antipruritic effect?? * Horses: photic head shaking, and PPID (kind of Cushings in horses) * Adverse effects: CNS and anticholinergic

Cyproheptadine

* 1st generation * Motion sickness and vestibular disease * MOA: partially understood * Antiemetic action through CRTZ (chemo receptor trigger zone)

Meclizine

Devoid of mineralocorticoid activity Group A/short acting o Duration of action dependent on salt formulation: • Sodium succinctness/solu-medrol • Water soluble form with rapid effect – emergency/acute tx • Acetate/depo-medrol (LONG acting)

Methyl-prednisolone (not really on list)

Serotonin overdose signs!!!

o Neuro signs: seizures, depression (mental dullness), tremors, hyperesthesia, and ataxia o GI signs: vomiting, diarrhea, abdominal pain, hypersalivation o Other: hyperthermia, blindness

Partial (mixed) agonist at mu agonist: kappa Good analgesic in dogs, cats, horses Effective anti-tussive in dogs and cats excitability in horses

Butorphanol

``` • Tricyclic antidepressant • Only FDA approved drug (dogs) • Tx of OCD, anxiety, and dominance aggression • Used off label in cats and birds Reuptake inhibitor (TCA) ```

Clomipramine

* Selective serotonin reuptake inhibitor * Doesn't cure problem * FDA approved in dogs for tx of separation anxiety in conjunction with behavior modification plan * Adverse effects: anorexia and seizures

Fluoxetine

* Atypical antidepressant * 5-HT2 and 5-HT3 inhibitor (acts on post synaptic cleft) * Central alpha 2 receptor inhibitor (net increase in NE) * Appetite stimulant * Antiemetic (anti-nausea) * Adverse effects: drowsiness/sedation, vocalization, tachycardia

Mirtazapine

* 5-HT2 inhibitor and SSRI * Adjunctive anxiolytic * Tx: hospitalization related anxiety and post op recovery * Adverse effects: GI signs, ataxia, hypotension? * Less cardiovascular effects, unlike Ace

Trazodone

* 5-HT4 agonist and enhances acetylcholine release from plexus * Enhances acetylcholine release * Prokinetic * Treatment of GI stasis, reflux esophagitis, constipation/megacolon (cats) * Well tolerated

Cisapride

* Serotonin receptor agonist * Potent antimetic, like cerenia * Receptors in vagal nerve terminals and CRTZ * Controversial use in cats * Well tolerated in dogs

Ondansetron (Zofran)

o Used in combination with a loop diuretic to treat refractory heart failure o Increase renal excretion of K and Mg o Reduce Ca and urate excretion Site of action: distal convoluted tubule

Hydrochlorothiazide

Spironolactone

o Exact mechanism not known but involves GABA o Acidic drug Moderately protein bound F is high, absorption slow Hepatic metabolism and some renal excretion Withdrawal symptoms will occur Induced liver enzymes increases metabolism of other drugs which decreases efficacy Can produce sedation, PU/PD, polyphagia Can make animal look hypothyroid, but will have a normal TSH

Phenobarbital

o Metabolized by liver o Related to sulfonamide antibiotics o Seizure frequency reduction as add on 70% Cat friendly!

Zonisamide

Technically blocks calcium channels to prevent neurotransmitter release ( Inhibits synaptic vesicle protein SV2A) Safe in cats and rabbits for anti-seizure medication

Levetiracetam

sedative/tranquilizer of benzodiazepine class; produces CNS depression by enhancing the inhibitory actions of the NT GABA Can be a Anti-seizure med

diazepam

medullary (brainstem) stimulant

doxapram

Psychomotor cortical stimulant respiratory stimulant tx of CNS associated hypoventilation

Caffeine

bronchodilator, is a methylaxanthines | can cause CNS over excitation

Theophylline

``` Most widely used across species little mineralocorticoid activity Group C/long acting rapid onset potent concern with colonic perforation and laminitis in the horse ```

Dexamethazone

o Group A/short acting | o 4-5x more potent than cortisol but has more mineralocorticoid activity than other synthetics

Prednisone

o Moderately insoluble ester, absorption over days to weeks

Fludrocortisone

Methyl-prednisolone (not really on list)

Alkaloid Agonist: Mu>>>delta=kappa High first-pass metabolism with slow GI absorption Metabolized via glucuronide conjunction (longer 1/2 life in cats and horses) Schedule II substance

Morphine

Partial (mixed) agonist at mu agonist: kappa Good analgesic in dogs, cats, horses Effective anti-tussive in dogs and cats

Butorphanol

Potent full agonist: Mu receptor o Good analgesic in dogs, cats, horses o Less CV impact than morphine o Fairly short half life (rapid liver metabolism)

fentanyl

antagonist: Mu>>>kappa>delta short 1/2 life Few uses except as reversal agent or treatment of opioid toxicity

Naloxone

Exam 2 Flashcards

(85 cards)