Term
|
Definition
Neutralize stomach acid (bind with protons) forming water and neutral salts
May stimulate PGE synthesis
May absorb bile
May inhibit pepsin |
|
|
Term
| How long do antacids work for? |
|
Definition
Short time
Minimal systemic absorption |
|
|
Term
| What are drug-drug interactions for antacids? |
|
Definition
Fluoroquinolones (bind and inactivate)
Tetracyclines (bind and inactivate)
Domperidone (absorbed better in acidic environment)
Digoxin (bind and inactivate) |
|
|
Term
| What are the specific drug names of antacids? |
|
Definition
Aluminum hydroxide
Magnesium hydroxide
Calcium carbonate (some systemic Ca2+ absorption) |
|
|
Term
| What is the mode of action of sucralfate? |
|
Definition
Dissociates to sucrose SO4 and AlOH
Sucrose SO4 forms viscous polymer creating a protective layer and binds to ulcerated tissue
Inactivates pepsin and bile
Increase PGE and EGF |
|
|
Term
| What is the bioavailability of sucralfate? |
|
Definition
|
|
Term
| What are the drug-drug interactions for sucralfate? |
|
Definition
Fluoroquinolones (Al bind and inactivate)
Tetracyclines (Al bind and inactivate)
Digoxin (Al bind and inactivate) |
|
|
Term
| What is the efficacy of sucralfate? |
|
Definition
|
|
Term
| What are the adverse effects of sucralfate? |
|
Definition
| None really (minimal PO absorption) |
|
|
Term
| What is the mode of action of ranitidine/cimetidine/famotidine? |
|
Definition
Bind to H2 receptors and decrease acid secretion
Increase gastric and colonic motility by inhibiting ACh-esterase activity |
|
|
Term
| How is ranitidine/cimetidine/famotidine elimitated? |
|
Definition
Hepatic
Renal (dz decreases clearance, increases GIT ADE) |
|
|
Term
| What is the specific drug-drug interaction of cimetidine? |
|
Definition
| CYP-inhibitor (so drug metabolism interactions) |
|
|
Term
| Are H2 antagonists well-tolerated? |
|
Definition
Yes!
Poor %F PO in horses (increase dose) |
|
|
Term
| What are the differences between ranitidine, cimetidine, and famotidine? |
|
Definition
Cimetidine 1x potency, short duraction
Ranitidine 10x potency, 8hr duration
Famotidine 50x potency, 8hr duration |
|
|
Term
| How do proton pump inhibitors work? |
|
Definition
| Irreversible inhibition of H+/K+ ATPase proton pump (decrease [H+]) |
|
|
Term
| Which acid suppressant has the highest efficacy? |
|
Definition
|
|
Term
| What is the mode of action of omeprazole? |
|
Definition
|
|
Term
| WWhat should you not do to omeprazole tablets? |
|
Definition
| Crush them! (breaks down in an acidic environment, needs to be absorbed systemically) |
|
|
Term
| EWhy aren't the effects of omeprazole predicted by its T1/2? |
|
Definition
Inhibition is irreversible
Drug accumulates in parietal cells |
|
|
Term
| What is the metabolism of omeprazole? |
|
Definition
|
|
Term
| What are the adverse effects of omeprazole? |
|
Definition
Diarrhea (most common)
Bacterial overgrowth (chronic admin)
Decreased absorption of ketoconazole, itraconazole, and domperidone (need acidic environment to be absorbed) |
|
|
Term
| What is the target pH for healing GI ulcers? |
|
Definition
|
|
Term
| What is the mode of action of misoprostol? |
|
Definition
|
|
Term
| What is the metabolism of misoprostol? |
|
Definition
|
|
Term
| What are the effects of PGE? |
|
Definition
Decrease stomach acidity
Increase mucous and bicarb secretion
Increase mucosal blood flow
Increase uterine contractions
Increase GIT motility |
|
|
Term
| What are the adverse effects of misoprostol? |
|
Definition
Diarrhea
Cramps
Abortion (in handlers too!) |
|
|
Term
| Which drug is more effective at preventing NSAID-induced ulcers than treating them? |
|
Definition
|
|
Term
| What is the T1/2 of misoprostol? |
|
Definition
| Short (3-4x daily dosing) |
|
|
Term
| What is the mode of action of bismuth subsalicylate? |
|
Definition
| Primary effect due to salicylate producing anti-inflammatory effect |
|
|
Term
| What are the adverse effects of bismuth subsalicylate? |
|
Definition
Aggravate NSAID ADE (aspirin metabolized to salicylate - "stacking")
Salicylate toxicity
Increased bleeding time
Stains stool black (not melena) |
|
|
Term
| What is sulfasalazine indicated for? |
|
Definition
|
|
Term
| What is sulfasalazine broken down into? |
|
Definition
Sulfapyridine (carrier)
5-aminosalicylic acid (mesalamine - active ingredient) |
|
|
Term
| What is the metabolism of sulfasalazine? |
|
Definition
|
|
Term
| What is the mechanism of action of sulfasalazine? |
|
Definition
|
|
Term
| What are the adverse effects of sulfasalazine? |
|
Definition
Sulfa - KCS, hypersensitivity, hepatotoxicosis (especially dogs)
Cats have trouble eliminating mesalamine |
|
|
Term
| Which neurotransmitters are associated with vestibular system emesis? |
|
Definition
Ach (M1)
Histamine (H1) (dogs) |
|
|
Term
| Which neurotransmitters are associated with GIT emesis? |
|
Definition
|
|
Term
| Which neurotransmitters are associated with vomiting center emesis? |
|
Definition
Serotonin (5HT3)
Norepi (A2)
Dopamine (DA2)
Opioid (inhibitory)
Sub P (NK1) |
|
|
Term
| Which neurotransmitters are associated with CRTZ emesis? |
|
Definition
Dopamine (DA2)
Serotonin (5HT3)
NE (A2)
Sub P (NK1) |
|
|
Term
| What drug are cats susceptible to emesis from? |
|
Definition
|
|
Term
| Which NT is most prominent in vestibular emesis in dogs? |
|
Definition
|
|
Term
| Which NT are dogs susceptible to emesis from? |
|
Definition
|
|
Term
| What are two examples of phenothiazine anti-emetics? |
|
Definition
Chlorpromazine (primary antiemetic)
Acepromazine (primary sedation) |
|
|
Term
| How do phenothiazines prevent vomiting? |
|
Definition
|
|
Term
| What are other effects of phenothiazines? |
|
Definition
A1 antagonist (vasodilation)
Antihistamine (H1)
Antimuscarinic |
|
|
Term
| What are the adverse effects of phenothiazines? |
|
Definition
Sedation (potentiate other sedatives)
Decrease seizure threshold
Hypotension (A1 antagonist too! Don't use in dehydration)
Epi reversal (due to A1 blockade) |
|
|
Term
| How are phenothiazines eliminated? |
|
Definition
|
|
Term
| What is the mechanism of action of aminopentamide? |
|
Definition
|
|
Term
| What is the mode of action of diphenhydramine? |
|
Definition
H1 receptor antagonist
Mild antimuscarinic |
|
|
Term
| How is diphenhydramine metabolized? |
|
Definition
|
|
Term
| What are the adverse effects of diphenhydramine? |
|
Definition
Sedation
Excitement (cats)
Antimuscarinic |
|
|
Term
| What is the mode of action of metoclopramide? |
|
Definition
DA2 antagonist
Prokinetic
5HT3 antagonist (high doses) |
|
|
Term
| What are the non-antiemetic effects of metoclopramide? |
|
Definition
Increase prolactin release (also domperidone)
Increase aldosterone release (Na, H20 retention) |
|
|
Term
| How bioavailable is metoclopramide? |
|
Definition
|
|
Term
| How is metoclopramide metabolized? |
|
Definition
|
|
Term
| What are the non antiemetic effects of metoclopramide? |
|
Definition
Increase gastric emptying
Incrase tone gastroesophageal sphincter
Increase duodenal motility (no effects on large intestine) |
|
|
Term
| What are the adverse effects of metoclopramide? |
|
Definition
Excitement
Exaceration of seizures
Abdominal pain
GIT rupture
Involuntary muscle movements
Aldosterone release (edema, CHF)
Prolactin release (lactation) |
|
|
Term
| What are contraindications for metoclopramide? |
|
Definition
Physical obstruction
GI foreign bodies
Hemorrhage |
|
|
Term
| How do serotonin antagonists work? |
|
Definition
Inhibits vagal afferent from intestines
Some activity at CRTZ |
|
|
Term
| What is the mechanism of action of ondansetron? |
|
Definition
|
|
Term
| What is the duration of effect of ondansetron? |
|
Definition
6-8 hours (short T1/2 but outlasts prediction due to high affinity for 5HT3)
Poor PO %F |
|
|
Term
| What is the mode of action of maropitant? |
|
Definition
|
|
Term
| What is the only antiemetic with once daily administration? |
|
Definition
|
|
Term
| How is maropitant metabolized? |
|
Definition
Hepatic (CYP - phase I)
Dose-dependent
Saturable
Recommended short-term admin due to accumulation |
|
|
Term
| What are the adverse effects of maropitant? |
|
Definition
Pain on injection
Diarrhea
Lethargy (NK1)
Ataxia/sedation
Anaphylaxis
Bone marrow suppression (young pups)
Prolonged QT interval (Class III and IV antiarrhythmic) |
|
|
Term
| What are the precautions with maropitant? |
|
Definition
Cardiac dz (diltiazem, amlodipine, sotalol)
Antiarrhythmic drugs
Doxorubicin (cardiotoxic antineoplastic) |
|
|
Term
| What are the drug-drug interactions for maropitant? |
|
Definition
Phenobarb - increases clearance (CYP)
Ketoconazole, itraconazole, cimetidine, fluoxetine, paroxetine, quinidine - decrease elimination
Saturable metabolism - careful with liver dz! |
|
|
Term
| Which classes of antiemetics should be used to treat motion sickness? |
|
Definition
Dogs: antihistamines, phenothiazines, maropitant
Cats: phenothiazines, maropitant |
|
|
Term
| Which classes of antiemetics should be used to treat drug-induced vomiting? |
|
Definition
| Maropitant, metoclopramide, phenothiazines |
|
|
Term
| Which classes of antiemetics should be used to treat GI vomiting? |
|
Definition
5HT3 antagonists
Phenothiazines
Metoclopramide
Maropitant
AVOID ANTIMUSCARINICS (decrease GI motility) |
|
|
Term
| What is the mechanism of action of domperidone? |
|
Definition
| DA2 antagonist (similar to metoclopramide) |
|
|
Term
| What is the elimination of domperidone? |
|
Definition
|
|
Term
| What is the difference between domperidone and metoclopramide? |
|
Definition
Domperidone less efficacy
Domperidone does not cross BBB (use in horses) |
|
|
Term
| What side effect of domperidone is used to treat fescue toxicosis in horses? |
|
Definition
| Enhances prolactin release (treats agalactia) |
|
|
Term
| What are the drug-drug interactions of domperidone? |
|
Definition
| Acid suppression therapy (needs acidic environment for absorption) |
|
|
Term
| What is the mechanism of action of cisapride? |
|
Definition
5HT4 agonist (myenteric neurons)
+/- 5HT3 antagonist
+/- ACh agonist (myenteric plexus) |
|
|
Term
| What is the main use for cisapride? |
|
Definition
| GIT prokinetic (upper and lower GIT motility) |
|
|
Term
| How is cisapride metabolized? |
|
Definition
|
|
Term
| What are the drug-drug interactions for cisapride? |
|
Definition
CYP 3A inhibitors (cisapride is a substrate)
-Ketoconazole
-Itraconazole
-Erythromycin
-Cyclosporine
-Cimetidine |
|
|
Term
| What are the adverse effects of cisapride? |
|
Definition
Abdominal pain
Arrhythmias (people - K+ channel blocker) |
|
|
Term
| What are stimulant (irritant) laxatives? |
|
Definition
Unknown mechanism
Rapidly acting
May cause excessive fluid/electrolyte loss |
|
|
Term
| What is the mechanism of action of hyperosmotic cathartics? |
|
Definition
Increase fluid content by osmosis
Quick onset of action |
|
|
Term
| What is the mechanism of action of hydrophilic colloids (bulk laxatives)? |
|
Definition
Nonabsorbed material resists digestion and attracts fluid
Increase mass and stimulate motility mechanically |
|
|
Term
| What is the mechanism of action of lubricant laxatives? |
|
Definition
|
|
Term
| What is the mechanism of action of stool softeners? |
|
Definition
Decrease stool surface tension
Increase fluid content
Emulsify fats/stool (keeps fat/fluid in stool) |
|
|
Term
| How long do stool softeners take to work? |
|
Definition
|
|
Term
| What is the main adverse effect of stool softeners? |
|
Definition
|
|
Term
| How do opioids stop diarrhea? |
|
Definition
Decrease GIT secretions
Decrease propulsive contractions
Increase non-propulsive contractions
Ileus |
|
|
Term
| What is the mechanism of action of loperamide? |
|
Definition
Mu opioid agonst
Does not cross BBB (p-gp excluded) |
|
|
Term
| How is loperamide metabolized? |
|
Definition
|
|
Term
|
Definition
Fluids and solute (ie salts)
Permeable through capillaries |
|
|
Term
|
Definition
Fluid with large polymers
Unable to permeate capillaries |
|
|
Term
| What types of fluids can be administers interosseous (IO)? |
|
Definition
|
|
Term
| What can NOT be administered IP? |
|
Definition
|
|
Term
| What types of fluids CANNOT be administered SC? |
|
Definition
|
|
Term
| In crystalloid solutions, what are lactate, acetate, and gluconate metabolized into? |
|
Definition
|
|
Term
| Is 0.9% NaCl acidifying or alkalinizing? |
|
Definition
|
|
Term
| Is LRS an acidifying or alkalinizing fluid? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| What are two common fluid additives? |
|
Definition
|
|
Term
| What type of drug penetrates the corneal epithelium? |
|
Definition
Surface epithelium - hydrophobic
Stroma - hydrophilic
Drug needs both to penetrate anterior chamber |
|
|
Term
| What type of drug penetrates the blood-aqueous, blood-vitreous, and blood-retinal barriers? |
|
Definition
Lipophilic
Low protein-binding |
|
|
Term
| What disease state decreases the blood-aqueous, blood-vitreous, and blood-retinal barrier? |
|
Definition
Inflammation
Increases drug penetration |
|
|
Term
| Why can you sometimes see systemic effects of drugs applied topically to the eye? |
|
Definition
| Drainage of nasolacrimal duct and swallowing |
|
|
Term
| What does aqueous humor do? |
|
Definition
| Provides nutrition to avascular structure of the eye (i.e. lens, cornea) |
|
|
Term
| How does glaucoma damage structures such as the retina and optic nerve? |
|
Definition
| Increased intraocular pressure leads to ischemia |
|
|
Term
| How can you decrease the outflow of aqueous humor? |
|
Definition
|
|
Term
| What is the underlying cause of glaucoma? |
|
Definition
|
|
Term
| What is the mode of action of timolol? |
|
Definition
| B antagonist (acts on ciliary body epithelium and vasculature) |
|
|
Term
| What are the adverse effects of timolol? |
|
Definition
Negative inotrope
Bradycardia
Hypotension
B2 block - brochoconstriction
AV block |
|
|
Term
| What are two examples of carbonic anhydrase inhibitors? |
|
Definition
Methazolamide - systemic
Dorzolamide - topical |
|
|
Term
| What is the mechanism of action of carbonic anhydrase inhibitors? |
|
Definition
Decrease aqueous humor production by inhibiting the conversion of CO2 to HCO3
Synergistic with B-blockers (timolol) |
|
|
Term
| What are the adverse effects of carbonic anhydrase inhibitors? |
|
Definition
Diuresis (weak)
Metabolic acidosis
Topical treatment as effective as systemic w/o the ADE! |
|
|
Term
| What is the mode of action of latanoprost? |
|
Definition
PGF2A analogue
Increases aqueous outflow
Causes miosis |
|
|
Term
| What is the main contraindication for latanoprost? |
|
Definition
| Uveitis (PGs enhance inflammation) |
|
|
Term
| What is the mechanism of action of pilocarpine? |
|
Definition
Muscarinic agonist
Miosis
Increase outflow of aqueous humor |
|
|
Term
| What is the mode of action of tropicamide? |
|
Definition
Antimuscarinic
Mydriasis ("tropicamide open wide") |
|
|
Term
| What is the mode of action of atropine? |
|
Definition
Antimuscarinic
Mydriasis
Control ciliary spasm/pain |
|
|
Term
| What are the adverse effects of atropine? |
|
Definition
Systemic antimuscarinic effects
Ileus in horses
Even when given topically! |
|
|
Term
| What is the mode of action of proparacaine/tetracaine? |
|
Definition
NA+ channel blockers
Anesthesia of cornea/conjunctiva ("proparacaine cure the pain") |
|
|
Term
| What is the main contraindication of proparacaine/tetracaine? |
|
Definition
| Corneal ulcers (inhibit healing and blink reflex) |
|
|
Term
| What topical corticosteroids are used for superficial inflammation (i.e conjunctivitis)? |
|
Definition
|
|
Term
| What topical corticosteroids are used for intraocular inflammation (i.e anterior segment)? |
|
Definition
Prednisolone acetate
Dexamethasone |
|
|
Term
| What is the mode of action of cyclosporine/tacrolimus? |
|
Definition
Calcineurin inhibitors
Inhibit T cell activation/proliferation |
|
|
Term
| What is the mode of action of amprolium (Corid)? |
|
Definition
Antiprotozoal
Coccidiostat
Competes for thiamine
Effective against 1st gen schizont
Preventive |
|
|
Term
| What is the mode of action of decoquinate (Deccox)? |
|
Definition
Antiprotozoal
Quinolone - kills sporozoite by disrupting electron transport in mitochondria |
|
|
Term
| What is the mode of action of sulfonamides? |
|
Definition
Antiprotozoal
Structural analog of PABA (inhibits dihydropterate synthetase in folic acid synthesis) |
|
|
Term
| What is the mode of action of monensin (Rumensin) or lasalocid (Bovatec)? |
|
Definition
Antiprotozoal
Complexes with Na and K ions, makes membranes permeable |
|
|
Term
| What is the use for ponazuril (Marquis)? |
|
Definition
Horses with EPM
Off-label for coccidia in other species |
|
|
Term
| What is the mode of action of imidocarb dipropionate? |
|
Definition
Antiprotozoal
Inhibits nucleic acid metabolism
Works on intracellular arthropod-borne organisms |
|
|
Term
| What is the mode of action of macrocyclic lactones? |
|
Definition
| Bind to glutamate-gated chloride channels |
|
|
Term
| What is doramectin (Dectomax) used for? |
|
Definition
Nematodes, lice, mites, grubs
Macrocyclic lactone
Long withdrawal |
|
|
Term
| What is eprinomectin (Eprinex) used for? |
|
Definition
Broad spectrum activity
No withdrawal |
|
|
Term
| What class of anthelmintic is ivermectin in? |
|
Definition
|
|
Term
| What is the consideration with milbemycin oxime? |
|
Definition
|
|
Term
| What species is moxidectin not approved for? |
|
Definition
|
|
Term
| What is selamectin (topical) effective for? |
|
Definition
| Internal nematodes and heartworm in CATS |
|
|
Term
| What is the mode of action of benzimidazoles (i.e. fenbendazole)? |
|
Definition
| Bind to tubulin molecules |
|
|
Term
| What is an example of a tetrahydropyrimidine? |
|
Definition
|
|
Term
| What is the mode of action of isoquinolones (i.e. praziquantel, epsiprantel)? |
|
Definition
| Attack the neuromuscular junction and the tegument |
|
|
Term
| What is the only arsenical available in the US? |
|
Definition
| Melarsomine dihydrochloride |
|
|
Term
| What are the broad spectrum antifungals? |
|
Definition
Amphotericin
Azoles
Terbinafine |
|
|
Term
| What are the narrow spectrum antifungals? |
|
Definition
|
|
Term
| Which antifungals treat Aspergillus? |
|
Definition
Amphotericin
Itraconazole
Voriconazole
Terbinafine |
|
|
Term
| What is amphotericin B a product of? |
|
Definition
|
|
Term
| What kind of molecule is amphotericin B? |
|
Definition
| Amphoteric polyene macrolide |
|
|
Term
| What is the mechanism of action of amphotericin B? |
|
Definition
| Binds to ergosterol in cell wall, increasing permeability |
|
|
Term
| What is the dose-limiting adverse effect of amphotericin B? |
|
Definition
|
|
Term
| What are the other adverse effects of amphotericin B? |
|
Definition
Tremors
Vomiting
Pyrexia
Anorexia
Phlebitis |
|
|
Term
| How is amphotericin B administered? |
|
Definition
IV (Poor %F PO)
Poor penetration to CNS, vitreous humor
Good penetration to aqueous humor |
|
|
Term
| How is amphotericin B eliminated? |
|
Definition
|
|
Term
| What is the mechanism of action of the azoles? |
|
Definition
Reduce ergosterol synthesis by inhibiting fungal CYP450
Cell wall damage |
|
|
Term
| What species cannot be given ketoconazole? |
|
Definition
|
|
Term
| What should ketoconazole be given with? |
|
Definition
|
|
Term
| How is ketoconazole metabolized? |
|
Definition
Hepatic
Fair penetration into CNS |
|
|
Term
| What are the adverse effects of ketoconazole? |
|
Definition
Nausea, anorexia, vomiting
Hepatotoxicity
Decrease cortisol
Cataracts
Hair coat lightening
CYP3A inhibitor/substrate
P-GP inhibitor |
|
|
Term
| What is the benefit of itraconazole over ketoconazole? |
|
Definition
Less adverse effects
Less resistance, higher efficacy
Nukes aspergillus
Treatment of choice |
|
|
Term
| What formulation of itraconazole should you NEVER use? |
|
Definition
|
|
Term
| How is itraconazole metabolized? |
|
Definition
Hepatic
Poor CNS penetration
NO horses |
|
|
Term
| Why is itraconazole effective for dermatophytes? |
|
Definition
High lipophilicity
Accumulates in stratum corneum |
|
|
Term
| What fungi does fluconazole have poor activity against? |
|
Definition
Aspergillus
Dermatophytes
Malassezia |
|
|
Term
| What is a major advantage of fluconazole? |
|
Definition
| Well absorbed orally (even horses) |
|
|
Term
| How is fluconazole eliminated? |
|
Definition
Renal
Good CNS penetration |
|
|
Term
| Which antifungal has the highest activity against aspergillus? |
|
Definition
|
|
Term
| What cells does voriconazole accumulate in? |
|
Definition
|
|
Term
| How is voriconazole eliminated? |
|
Definition
Hepatic
Penetrates into CNS and aqueous humor |
|
|
Term
| What are the adverse effects of voriconazole? |
|
Definition
Hepatotoxicity
Visual disturbances
Rash |
|
|
Term
| What is the mode of action of terbinafine? |
|
Definition
| Inhibition of squalene epoxidase which decreases ergosterol synthesis |
|
|
Term
| What fungus does terbinafine not work on? |
|
Definition
|
|
Term
| How is terbinafine eliminated? |
|
Definition
Hepatic
Poor CNS penetration |
|
|
Term
| What are the adverse effects of terbinafine? |
|
Definition
Vomiting
Anorexia
Hepatitis |
|
|
Term
| What is the mechanism of action of griseofulvin? |
|
Definition
Inhibits fungal mitosis
Deposited in keratin of skin
Not for systemic use |
|
|
Term
| What is griseofulvin good for? |
|
Definition
|
|
Term
| What should you give griseofulvin with? |
|
Definition
|
|
Term
| How is griseofulvin metabolized? |
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Definition
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Term
| What are the adverse effects of griseofulvin? |
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Definition
Teratogen
Anemia and leukopenia in FIV cats
Anorexia, depression, vomiting, diarrhea |
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