Professional Documents
Culture Documents
- use: relief of pain, analgesia for minor - synthetic, equipotent to morphine - controlled substance; partial agonist w very high
surgery, cough suppression, tx of - Ix: severe pain, COLIC (horses) affinity for mu receptors
secretory diarrhea - produces LESS sedation than morphine -10-20x more potent than morphine
- PK: readily absorbed, distribute (but not persist) Meperidine (pethidine: UK) - LONG-TERM analgesia (8-10 hours post-op)
in parenchymatous tissues - synthetic, mu agonist - cause LESS sedation and respiratory depression
Undergoes glucuronidation - controlled substance *reversed with NALOXONE
BENZIMIDAZOLE
Diminazene diaceturate, Pentamidine isethionate,
Trimethoprim – coccidiosis, neosporosis,
Phenamidine isethionate
toxoplasma, malaria
Imidocarb diproprionate – Ix: Babesia sp.
Ormethoprim + sulfadimethoxine – px of
- Ix: Giardia sp. coccidiosis
- Adv Pyrimethamine
fx: teratogenic – toxoplasmosis
Fenbendazole, albendazole
ANTHELMINTICS: ANTINEMATODAL DRUGS TETRAHYDROPYRIMIDINES Birds, snakes – endoparasites
BENZIMIDAZOLES - MoA: mimic action of Ach (cholinergic agonist) - Adv fx: in Collies/collie crosses*, Murray Grey cattle
- MoA: interfere with energy metabolism of worn → worm paralysis *MDR1/ABCB1 gene mutation for p-glycoprotein
- Activity: broad spectrum - Ix: Horses – ascarids, strongyles, efflux transporter [supposedly prevents entry of ivermectin
- Ix: Horses – strongyles, pinworms, ascarids pinworms Cattle, sheep, goat – in BBB] → CNS depression, ataxia, possible death
Cattle – ascarids, several strongyle strongyle
species Dog, cat – hookworms, roundworms ANTICESTODES
liver fluke & tapeworms (albendazole) Swine – roundworms, strongyle PYRAZINE DERIVATIVES
lungworm (fenbendazole) Pyrantel pamoate/embonate, pyrantel tartrate, - MoA: ↑ permeability of worm’s cell membrane
Sheep, goat – ascarids, several strongyles, morantel tartrate → disintegration of cestode
stomach worms, lungworm Praziquantel – against all cestodes
(fenbendazole) IMIDAZOTHIAZOLES Adv fx: lethargy, vomiting, diarrhea, anorexia
Dog – hookworms, roundworms, pinworms, Epsiprantel – Taenia, Dipylidium sp.
- MoA: mimic action of Ach (cholinergic agonist)
Some effective against T. pisiformis, → worm paralysis
but not D. caninum - Activity: ascarid, whipworm, hookworm, ANTITREMATODAL DRUGS
Swine – strongyle, lungworm, strongyle (horse, cattle, sheep, goat,
lungworm Snakes, birds dog, cat, swine)
- Admn of repeated dose – advantageous - with immunostimulant, anti-inflammatory effects
(slow killing process) - Adv fx: cholinergic – salivation, ataxia, mm tremors
- Adv fx*: lethargy, vomiting, diarrhea, hepatotoxicity** - Formula: PO (pellet, powder, paste, susp.)
*uncommon; **mebendazole Levamisole, tetramisole
Albendazole, thiabendazole,
oxibendazole, mebendazole,
PIPERAZINES
cambendazole, oxfendazole, fenbendazole
- MoA: muscle hyperpolarization → block
*PROBENZIMIDAZOLES
neuromuscular transmission in parasite
- prodrugs
→ worm paralysis
Febantel – transformed into fenbendazole
Netobimin – transformed into albendazole - Activity: nematodes; cat and dog roundworms,
exotic animals (birds, snakes)
Clorsulon
- MoA: inhibit worm enzyme system → ↓energy
- Ix: adult, immature F. hepatica (cattle)
Albendazole
- MoA: interferes with worm’s energy metabolism
- Ix: adult F. hepatica (cattle)
- NOT approved for LACTATING (no
established withdrawal time)
Praziquantel
- Ix: lung trematodes (cats, dogs)
ORGANOPHOSPHATES - Formula: PO
HEARTWORM DISEASE
- MoA: inhibit acetylcholinesterase → worm paralysis Piperazine dihydrochloride, piperazine sulfate ADULTICIDES
- Activity: nematodes, bots - Thiacetarsamide – nephrotoxic, hepatotoxic,
- Ix: Horse – bots, strongyles, roundworms, pinworms AVERMECTIN coughing, gagging, lethargy
- Melarsomine – nephrotoxic, hepatotoxic (safer and more
Cattle – strongyles - Source: Streptomyces avermitilis effective than thiacertsamide), coughing, gagging,
Dog, cat – hookworms, roundworms, - MoA: bind to glutamate-gated Cl channels in depression, lethargy, anorexia, fever, vomiting
*Given deep IM epaxial (between L3-L5, once for 2 days)
whipworms Swine – ascarids, whipworms, neurons, myocytes → worm paralysis,
nodule worms, death MICROFILARICIDE
- PK: Does NOT cross BBB (unless at high dose) Ivermectin (50mcg/kg), Milbemycin, Levamisole
strongyles
- narrow margin of safety - Activity: broad spectrum; ruminants, horse, pig, dog PREVENTIVES
- OD → muscarinic, nicotinic signs in the host *also affect HEARTWORM LARVAE, ECTOPARASITES -Ivermectin – not for puppies < 6 weeks, collies/collie
Ivermectin, moxidectin, doramectin, selamectin, mixes; Adv fx: ataxia, depression, salivation
(SLUDGE → Salivation, Lacrimation, Urination,
- Milbemycin – also heartworm preventive (cats);
Diarrhea, GI Upset, Emesis) eprinomectin, milbemycine oxime* hookworms, ascarids, whipworms
*structurally related to avermectin
- Adv fx: muscle tremors, miosis - Selamectin – also fleas, ear mites, sarcoptic mange
IVERMECTIN (dogs) nematodes, hookworms (cat)
Dichlorvos, trichlorfon, coumaphos, haloxon
- Ix: Horse – strongyle, pinworm, ascarid, - Moxidectin – 6-month injection
OT Plus (mebendazole + trichlorfon) Adv fx: GIT signs, neurologic signs
hairworm, stomachworm, threadworm,
→ tx of parasitic infection caused by gastric bots - Diethylcarbamzine (DEC) – ascarids, hookworm,
bots, lungworm whipworm; Adv fx: vomiting
(Gastrophilus spp)
Cattle – GIT roundworm, lungworm, grub, lice,
mange mites
Dog, cat – preventive (D. immitis), hookworms
ANTIFUNGALS AZOLES SUPERFICIALS
- MoA: cause leakage of fungal cell membrane - MoA: disrupt fungal cell division
- Ix: systemic & superficial mycoses - Ix: topical/superficial
- Activity: broad spectrum; delayed onset of effect mycoses; targets
(Trichophyton verrucosum, T equinum, T mentagrophytes, dermatophytes
Microsporum canis, M nanum; yeast: Malassezia
pachydermatis, Crpytococcus neoformans)
- Form: PO, topical forms
- Adv fx: hepatotoxic, teratogenic
Dogs – inappetence, vomiting, pruritus,
alopecia, reversible lighting of hair coat
Cats* - anorexia, fever, depression,
diarrhea,
POLYENES ↑liver enzymes, hepatotoxicity
- MoA: bind to ergosterol* → disrupt fungal cell Ketoconazole, miconazole, itraconazole,
membrane (form pores → clotrimazole
leaky) Ketoconazole – administer with food
*membrane lipid of fungi → reduce side effects
Nystatin Miconazole – broad spectrum; topical formula
- Ix: oral, GIT C. albicans infection (dog, cat, bird) Clotrimazole – broad spectrum; topical formula
- Form: oral, topical Itraconazole
- Adv fx: GI upset, hypersensitivity - MoA: > potency, ↓ toxicity, wider spectrum
Amphotericin B than ketoconazole
- systemic antifungal - Ix: systemic mycoses
- Ix: progressive, disseminated deep mycosis - DoC for BLASTOMYCOSIS
- Forms: IV (store in dark), topical forms - Forms: oral, IV
- PK: poor GI absorption; good parenteral (IV) Fluconazole
penetration (except into muscle, bone, - Ix: tx of CNS MYCOSES, fungal and
eye, synovial fluid) yeast infections
- Adv fx: extremely nephrotoxic (dilute in *limited use in small animals
5% dextrose → reduce - Forms: PO, IV, topical formulations
*combination with amphotericin B: serious systemic
nephrotoxicity) disease; less nephrotoxic
*Lower dose recommended in cats (sensitive)
*diphenhydramine (0.5mg/kg IV), aspirin (10mg/kg PO), or
hydrocortisone Na succinate (0.5mg/kg IV) given before ANTIMETABOLICS
administration – reduce severity of side effects
- MoA: interfere with RNA & protein synthesis
In combination with: - PK: well-absorbed PO
- Rifampin – potentiates effect of amphotericin on - Adv fx: bone marrow suppression
Aspergilllus, Candida, Histoplasma
- Flucytosine – tx of Candida, Cryptococcus
Terbinafine
- MoA: interferes with fungal sterol biosynthesis
at an early stage, causing deficiency of
ergosterol, intracellular accumulation of
squalene, fungal cell death
- dosage (cats): 10-30mg/kg/day
- forms: PO, topical
Griseofulvin
- Adv fx: teratogenic in all species
Dogs – vomiting, diarrhea,↑liver enzymes
Cats – anemia, leukopenia, vomiting,
diarrhea, depression, pruritus, fever, ataxia
Bone marrow suppression (usually manifests
as neutropenia) – occur idiosyncratically,
especially in FIV-positive cats and kittens*
*determine FIV status before use; avoid in kittens <8 wk old
Flucytosine – effective against yeast
(Cryptococcus neoformans)
*synergistic with Amphotericin B – tx of Cryptococcus sp.
infections
PHENICOLS LINEZOLID NITROFURANS
(chloramphenicol, thiamphenicol, florefenicol) - MoA: 50s → (-) initiation process of protein synthesis - MoA: inhibit bacterial enzyme systems
- MoA: bind to 50s ribosomal subunit - PK: well absorbed, high bioavailability - Effect: bactericidal
- Effect: usually bacteriostatic - Ix: G+ (drug-resistant enterococcus, Staph, pneumo); - Activity: broad spectrum
(chloramphenicol – bactericidal at high tx multidrug-resistant infection (humans)
conc’n) - PK: excreted unchanged; rapid elimination
- Activity: broad spectrum - Ix: UTI
(G+, G-, Rickettsia spp., Chlamydia spp.,
QUINOLONES - Adv fx: GIT, hepatic disturbance
Enterobacteriaceae, anaerobes) - MoA: inactivate DNA gyrase* for DNA replication Nitrofurantoin – UTI, wounds
*Florfenicol – contains fluorine → ↑ efficacy, ↓ toxicity, ↓ bacterial *DNA gyrase (topoisomerase II) for supercoiling DNA Furazolidone – topical and ocular infections
resistance - Effect: Bactericidal Nitrofurazone
- PK: readily absorbed into tissues when administered - Activity: Broad spectrum *Banned in food producing animals → potential carcinogenic
*milk interferes with oral absorption of florfenicol - PK: rapid absorption PO, parenteral
50% plasma concentration of - Ix: local, systemic infections including those
chloramphenicol reaches CNS, ocular NITROIMIDAZOLES
caused by intracellular pathogens - MoA: disrupt DNA, nucleic acid synthesis
tissues, (less for florfenicol) Flumequine, nalidixic acid
Hepatic metabolism - Effect: Bactericidal
Urinary, biliary excretion - Activity: antibacterial (anaerobic), antiprotozoal
FLUOROQUINOLONES effects (Giardia, Trichomonas,
Cats: plasma half-life longer due to lack
- newer generation of quinolones amoebiasis)
of glucuronyl transferase
- MoA: inhibit DNA gyrase - CIx: PREGNANT
Chloramphenicol
*bound to fluorine → better potency, absorption, - Adv fx: anorexia, vomiting,
- Ix: systemic, local infections (SALMONELLOSIS,
broader spectrum diarrhea, neurologic signs
Bacteroides sp.)
- BANNED in food producing animals → dose - Effect: Bactericidal Metronidazole – DoC for canine DIARRHEA
dependent bone marrow suppression, irreversible - Activity: good against G- AMINOCOUMARINS
aplastic anemia (Enterobacteriaceae); variable - MoA: inhibit DNA synthesis, RNA synthesis, cell
Florfenicol against G+ wall synthesis, protein synthesis
- Ix: tx of bovine respiratory diseases *MRSA resistant to fluoroquinolones
- less likely to produce blood dyscrasias - Effect: Bactericidal/static
- PK: good oral absorption, complete IM
- Adv fx: diarrhea, inappetence, ↓ water - Activity: mainly G+
absorption Renal excretion
consumption - Ix: treatment of BOVINE MASTITIS*
- Ix: for pet birds and exotics, tx for infections *in combination with other agents
- milk interferes with oral absorption
in ornamental fish and aquaculture Novobiocin, clorobiocin
Thiamphenicol
- Adv fx: cartilage lesions in growing dogs;
- Activity similar to chloramphenicol
- less toxic than chloramphenicol high dose → retinal blindness in
cats RIFAMYCIN
STREPTOGAMINS Enrofloxacin*, difloxacin, marbofloxacin, - MoA: bind to subunits of sensitive DNA-
- 2 Groups: Group A – virginiamycin M, danofloxacin, ciprofloxacin dependent RNA polymerase → disrupts
*fluoroquinolone-resistant strains of Campylobacter sp. (poultry) RNA synthesis
dalfopristin Group B – virginiamycin S,
quinupristin - Effect: Bactericidal
*To discourage bacterial resistance: use as a reserve - Activity: Broad spectrum;
- Effect: Bacteriostatic (independent); -cidal (combo)
drug, limit use to intractable G- bacterial infections effective against intracellular organisms
Dalfopristin/quinupristin – for vancomycin-resistant
Staphylococcus and Enterococcus faecium (humans) *(G+, some mycobacteria, few G- (mostly
cocci), some anaerobes, chlamydiae, fungi)
Virginiamycin (M + S)
Rifampin, rifamycin, rifadin
- growth promotant in chicken, turkey, swine, cattle
Rifampin + erythromycin – tx of R. equi infxn (foal)
- prevent NECROTIC ENTERITIS (C.
perfringens), COCCIDIOSIS; Tx and control
SWINE
TETRACYCLINES MACROLIDES LINCOSAMIDES
- Source: Streptomyces auerofasciens, S. - MoA: bind to 50s ribosomal subunit - MoA: bind to 50s bacterial ribosomal subunit
rimosus; some are semi-synthetic - Effect: Bacteriostatic, Bacteriocidal (at high doses) - Effect: bacteriocidal/bacteriostatic (depends on
- Effect: Bacteriostatic - Adv fx: cross-reaction may occur macrolide ATBs drug concentration, bacterial species)
- Activity: Broad-spectrum* - PK: Basic compound; good PO absorption - Activity: moderate spectrum
*G+, G-, little activity against E. coli, Salmonella, Proteus,
Pseudomonas; Mycoplasma, some Mycobacteria, Chlamydia, Distributes well to body tissues (not (G+ aerobic, anaerobic, some Mycoplasma sp.)
Ricketssia, Protozoa (Entamoeba histolytica, Giardia lambia, CNS); - PK: basic compound (ion trapping in udder, prostate)
Plasmodium falciparum, Trichomonas spp, T. gondii) effective for intracellular pathogens (e.g. Mycobacteria) High lipid solubility, largely distributed
- MoA: reversibly bind, distort 30s → prevent - Ix: Mycoplasma infection (pig, poultry), hemorrhagic Hepatic metabolism
addition of amino acids to peptide chain → block digestive disease (pigs), liver abscess (F. Binding to plasma proteins
translation necrophorum – cattle), respiratory infection (cattle) - Ix: Swine – dysyntery, mycoplasma
- Adv fx: TETRACYCLINE TEETH, Colitis Erythromycin infection, erysipelas, streptococcal
(horse), photodermatitis - source: Streptomyces erythreus infections
- Ix: Borreliosis, Brucellosis, Chlamydiosis, - activity: broad spectrum (Strep, S. aureus, Ruminant – intramammary infusion for mastitis
Ehrlichiosis, Leptospirosis, Listeriosis, penicillin-resistant strains, G-, obligate Dogs, Cats – abscess
Rickettsiosis, Tularemia, Anaplasmosis, anaerobes) Osteomyelitis, periodontal disease, soft
Psittacosis; GI, respiratory, skin, genito- - Adv fx: gastric irritation → vomiting tissue/wound infection involving G+ cocci,
urinary, sepsis, infectious ds of locomotive - alternative to PCN, DoC for Campylobacter, anaerobic
organs Rhodococcus equi - Adv fx: serious GI problems (fatal enterocolitis –
- Formulation: PO, ointment horses and other herbivores e.g. rabbit, rodent)
- CIx: PREGNANT, neonates up to 4
weeks (bone deformation, defect of Lincomycin
Tylosin
enamel) - source: Streptomyces lincolnensis
- in livestock; Mycoplasma, S. hyodysenteriae,
Naturally-occurring: chlortetracycline, - Clindamycin – derivative of lincomycin; indicated
G+ aerobes
oxytetracycline, tetracycline in Staphylococcal osteomyelitis
- cause FATAL DIARRHEA in horses Lincomycin-Spectinomycin
Semi-synthetic: doxycycline, minocycline - feed, water additive
PK: oxytetracycline, tetracycline, chlortetracycline - Formulations: oral, injectable
Irritating when given IM; rapid IV in cattle → PLEUROMUTILINS
cardiovascular collapse Tilmicosin - used exclusively in animals (esp. swine)
Variable absorption in GIT - Ix: bovine, ovine tx for respiratory ds. of - MoA: bind to 50s
Absorption impaired by milk, antacid, Ca, Mg, Zn Mannheimia haemolytica, Pasteurella sp.; - Effect: bacteriostatic; may be bactericidal
*Avoid milk, antacids, iron, salts 3 hours before & after Ovine mastitis due to S. aureus, M. - Activity: broad spectrum (G+, G-, anaerobes,
Excreted in urine agalactiae; A. pleuropneumoniae, M. mycoplasma)
PK: doxycycline, minocycline hypopneumoniae, P. multocida (pigs) Tiamulin
Lipophilic (lipid soluble), better PO absorption - Stays in body for 3 days - PK: lipophilic, weak base
Less affected by milk, Ca salts - Adv fx: tachycardia, swelling at injection site Cellular penetration, concentrated in milk
Better distribution (e.g. bronchial secretion, - Fatal if injected IV in primates, goat, horse, swine Rapid absorption PO in pre-ruminant calves,
prostatic fluid) monogastric animals (inactivated in rumen flora
Other macrolides PO)
DC – penetrates BBB, CSF; enters enterohepatic
Azithromycin, clarithromycin – for human medicine Tiamulin, Valnemulin
circulation via bile → Colitis in
Spiramycin – similar spectrum of activity as - exclusive in swine
horses erythromycin; has activity against T. gondii, - Ix: mycoplasma pneumonia, swine
MC – metabolized before biliary excretion Isospora sp. dysyntery, proliferative ileitis,
Excreted in feces; safer for animals w renal Josamycin leptospirosis
problems Kitasamycin - as feed additive
- combination with ionophores (e.g.
salinomycin, monensin) – myotoxicity,
Tigecycline *used in humans
- glycylcycline, derived from minocycline
- broader spectrum (MRSA, Enterococcus, multi-
resistant Enterobacteriaceae)
- Only IV
- PK: Absorption – good absorption PO - Effect: bacteriostatic - PK: diffuses well into body tissues
Distribution – body tissues, placenta, milk More rapidly cleared from plasma than
*few enter CSF, synovial fluid sulfonamides
* >80% protein binding ↑ half-life Distributed throughout body, including CSF
Biotransformation – liver (acetylation) Hepatic metabolism, Renal excretion
*dogs: unable to acetylate sulfonamides - Ix: Bacterial arthritis (pigs), prevention & tx of
Excretion: renal coccidiosis (chicken, turkey), colibacillosis
- Ix: Coccidiosis, Infectious coryza, Bacterial (chicken, livestock), Enteric septicemia
cystitis, Diptheria, Fowl Cholera, Fowl Typhoid, (CATFISH), Bacterial enteritis, EQUINE
Bacterial enteritis, Bacterial pneumonia, PROTOZOAL MYOENCEPHALITIS, Fowl
Pododermatitis, Pullorum disease, Bacterial cholera tx/px, Furunculosis (salmon, trout),
respiratory infection, skin & soft tissue Bacterial GIT infections, Infectious coryza, Mastitis,
infection Perioperative infections, Bacterial pneumonia,
- Adv fx: Crystalluria* Pododermatitis, Respiratory tract infections, skin and
Dogs: KCS, idiosyncratic toxicosis (eg soft tissue infections, STRANGLES, UTI
Doberman Pinschers), inhibition of Adv fx: crystallization in urinary tract hypersensitivity
thyroid hormone synthesis Horse: Blood dyscrasias
Horse: severe cardiac arrhythmia, collapse Dogs: KCS, idiosyncratic toxicosis (eg
(if administered with sulfonamide + Doberman Pinschers), inhibition of
sedative/anesthetic) thyroid hormone synthesis, neurologic
Poultry: hemorrhagic syndromes**, ↓ egg disorders – ataxia, aggression,
production, ↓ growth behavioral changes, polyarthritis, etc.
*sulfonamides insoluble in acidic urine → prevent by 1) maintaining
Combinations*:
high urine flow, 2) hydrate animal 3) alkalinize urine if necessary
**Vit K antagonism - trimethoprim-sulfadiazine (cotrimazine)
Sulfachlorpyridazine, sulfadimethoxine, sulfamerazine, - trimethoprim-sulfadoxine
sulfamethazine, sulfaquinoxaline, sulfanilamide, - trimethoprim-sulfamethoxazole (co-trimoxazole)
sulfathiazole, sulfadiazine, sulfadimidine (sulfamethazine), - trimethoprim-sulfaquinoxaline
sulfadimerazine, sulfadoxine, sulfafurazole, sulfaguinidine, - trimethoprim-sulfadiazine
*usually 1 part trimethoprim/ormetoprim + 5 parts sulfonamide
sulfadimethoxazole
POTENTIATED SULFONAMIDES
(sulfonamides + diaminopyridines) AMINOGLYCOSIDES
Diaminopyrimidines - Source: Streptomyces sp. (streptomycin, neomycin)
- Source: synthetic Micromonospora sp. (gentamicin, netilmicin)
- MoA: dihydrofolate reductase inhibitors* - MoA: binds to 30s ribosomal sub-unit → disruption of
*inhibits conversion of dihydrofolic acid to
tetrahydrofolic acid normal bacterial protein synthesis → cell death
- Effect: bacteriostatic - Activity: broad spectrum* (except streptomycin)
Ormetoprim, trimethoprim, baquiloprim *good for aerobic G- (e.g. Klebsiella, P. aeruginosa, E. coli),
*sulfonamide-diaminopyrimidine combination block sequential some G+ (e.g. S. aureus), mycobacterium, mycoplasma,
stages in synthesis of bacterial folic acid (tetrahydrofolate) spirochetes; ineffective against anaerobic bacteria
*synergistic antibacterial action *resistance to aminoglycoside: plasmid-mediated enzymes
- Activity: broad spectrum (G+, G-,
Chlamydophila, nocardia, some
protozoa (Toxoplasma spp.), some
anaerobes
- PK: active in alkaline media
Poor GI absorption (except neomycin); IM or
IV Low PP binding; distribute to ECF
Poor distribution in CSF, eye, brain, milk
Excreted unchanged in urine
*accumulate in proximal tubules, ear due to high phosphatidylinositol
- Adv fx: Nephrotoxic (neomycin – most; strepto- – least)
Ototoxic* (damage cochlear sensory, vestibular cells)
*avoid administration with ototoxic drugs (e.g. loop diuretics)
Neuromuscular blockade*
*↓ Ach release, sensitivity → curare-like paralysis
reversal agent: Ca gluconate or
neostigmine
- Avoid administration in animals with myasthenia gravis
- Ix: Septicemia, Digestive, Respiratory, Urinary ds*
*toxic AGs (e.g. neomycin): topical, oral
*less toxic AGs (e.g. gentamicin): parenteral (G- aerobes)
Streptomycin, dihydrostreptomycin, neomycin,
kanamycin, amikacin, gentamicin, tobramycin
*Synergism w B-lactam ATB: Penicillin G salts+dihydrostreptomyins
- induce acute hepatitis at high dosage
SPECTINOMYCIN
- Source: Streptomyces spectabilis
- Effect: Bacteriostatic
- Activity: Effective against G+, G-,
Mycoplasma; ineffective against
G- anaerobes
- MoA: bind to 30s, inhibit CHON synthesis
- PK: Minimal GI absorption, rapid IM absorption
Excreted unchanged in urine
- Adv fx: lacks toxic effects of
aminoglycosides May cause
anaphylactic reactions,
neuromuscular blockade
Lincomycin-spectinomycin
- Ix: tx of enteric, respiratory infections in livestock
- Lincomycin – G+; marginally enhance
spectinomycin’s activity against
mycoplasma, Lawsonia intracellularis
- Spectinomycin – G-
CARBAPENEMS (PENEMS) - Veterinary applications: BACITRACIN
- Source: thienamycin (from Streptomyces cattleya) Cattle – colibacillosis, salmonellosis, mastitis - Source: Bacillus subtilis var tracy
- broadest spectrum among B-lactam ATBs Swine – neonatal porcine colibacillosis - Activity: G+, few G-, some spirochetes
- MoA: can penetrate porin channels of bacteria - Effect: bactericidal*
Horse – bacterial keratitis/metritis by Klebsiella
- Ix: “last resort” ATB, bacterial infections resistant *requires divalent cations (e.g. zinc)
Dog, cat – local tx (bacterial keratitis, otitis
to other ATBs - MoA: interferes with cell wall synthesis
externa, skin infections)
- PK: poor GIT absorption, (prevents bactoprenol dephosphorylation
parenteral administration Poultry – colistin used in China for G- infections → (X) new monomers into growing cell
- NOT APPROVED for VETERINARY USE Polymyxin B
wall → lysis
Impipenem, meropenem, doripenem, ertapenem - usually combined with neomycin & bacitracin - PK: poor oral absorption (PO only for local
*Imipenem/cilastatin in topical preparations* (for broader spectrum) effect) Not used systemically
- cilastatin decreases imipenem hydrolysis in renal tubules *skin, mucous membrane, eye, ear infections
- PO in intestinal infections Parenteral → nephrotoxicity
- bowel sterilization prior to abdominal -often combined with neomycin & polymyxins to
MONOBACTAMS enhance antibacterial spectrum
surgery, irrigation solutions to flush
- MoA: bind to PBPs → disrupt bacterial cell wall - Topical – for wounds, as ointments
peritoneal cavity
- Activity: narrow spectrum ATB (wide range - used against necrotic enteritis in poultry
of aerobic G- bacteria; little G+
effect) GLYCOPEPTIDE ANTIBIOTICS
FOSFOMYCIN
(vancomycin, teicoplanin, avoparcin)
- Ix: G- BACTERIAL MENINGITIS - source: Streptomyces fradiae →
- NO CROSS-SENSITIVITY with B-lactam ATBs - Activity: G+ bacteria (G+ cocci)
produce fosfomycin, a
- PK: enters CSF after systemic administration Vancomycin
- Source: Streptomyces orientalis phosphonic acid
- Epileptogenic effects
- Effect: bactericidal - Effect: bactericidal
Aztreonam – for serious bacterial infections
- MoA: binds to pentapeptides of peptidoglycan - Activity: broad spectrum (G+, G-)
resistant to aminoglycosides or fluoroquinolones
monomers → inhibit peptidoglycan - MoA: cell wall inhibitor (irreversible inhibition
polymerization → inhibits cross-linking → of pyruvyl transferase*)
PEPTIDE ANTIBIOTICS
(polymyxins, Glycopeptides, Bacitracin, Fosfomycin)
weakens cell wall *enzyme catalyzing first step of peptidoglycan synthesis
PK: given IV (poor oral absorption, painful IM) - Low toxicity
*narrow TI if given parenterally Oral Fosfomycin: UTI (E. coli, E. faecalis) in humans
POLYMYXIN Adv fx: nephrotoxicity, ototoxicity - unlikely approved for food animals due to its
- source: Bacillus polymyxa - effective against MRSA (VRE is a public health concern) value of treating multidrug resistant bacteria in
- 2 forms used clinically: *not included in OIE veterinary antibiotics humans
*last resort
Polymyxin B (from B. polymyxa) – topical *prohibited by FDA in food-producing animals for fear of VRE - limited use in intensive production of broilers, pigs
Polymyxin E/Colistin (B. colistimus) – oral Teicoplanin
- MoA: disrupt structure of cell - resistance-resistant drugs SULFONAMIDES
membrane phospholipid; detergent- - Adv fx: hypersensitivity skin reactions, painful - Source: synthetic
like action → permeability changes IM, phlebitis (rarely nephro/ototoxicity – px - Activity: broad spectrum
→ cell death also
G+, G-, Chlamydia, some protozoa
receiving aminoglycosides)
- Activity: mostly G- (but does not affect Proteus (e.g. coccidia, toxoplasma)
- may be given rapid IV
spp, Serratia spp.) Avoparcin Ineffective against most obligate anaerobes
- Effect: Bactericidal - ATB growth promoter in poultry, swine – banned - Effect: bacteriostatic
- PK: not absorbed PO or topical (colistin sulfate due to residue and resistance issues - widespread resistance
PO used for local antibiotic effect) - regarded as anti-metabolite*
undergoes urinary excretion *inhibitor of metabolic process
Systemic use → nephrotoxicity, neurotoxocity, - MoA: inhibits dihydropteroate synthase (pteridine) →
neuromuscular blocking effects interfere with synthesis of bacterial folic acid*
*Activity DECREASED in presence of pus *important for DNA, RNA synthesis
*Blood, pus, tissue debris DECREASE antibacterial action
- (+) Cross sensitivity: hypersensitivity
ANTIBIOTIC THERAPY PENICILLINS - Ix: respiratory, skin, soft tissue infections, UTIs,
- DoC in horse, cattle; limited use (AMR) in small osteomyelitis, pre/post-op
- Dosing: units - Adv fx: hypersensitivity, cross-sensitivity with PCNs,
- PK: poor oral absorption (hydrolyzed by gastric acid) vomiting, diarrhea, loss of appetite,
superinfection Low to moderate plasma protein binding - Species consideration: same as B-lactam
ATBs;
concentrations in kidney, synovial fluid, liver, crosses placenta & distribute into
milk lung, skin, soft tissues
Not penetrate BBB, may treat CNS infections at 1ST Generation
high doses - Activity: greater activity against G+ bacteria,
Natural PCNs moderate G- activity (E. coli, Shigella,
- extracted, purified from mold cultures Enterobacter, Klebsiella, Pasteurella, Proteus,
- narrow spectrum Salmonella)
- Activity: some G+ (staph, strep) - Susceptible to cephalosporinase
Selected G- (arcanobaterium, 2nd Generation
L. - Activity: active against G+, G-
monocyotogenes, P. multocida) - more resistant to B-lactamases
Withdrawal period if not stated:
Penicillin G: degraded by stomach acid - Ineffective against: enterococci, Actinobacter spp.
Meat: 28 days
- Penicillin V: more stable for PO P. aeruginosa, many obligate anaerobes
- Milk, eggs: 7 days
Aminopenicillins (except cefoxitin)
- semisynthetic derivatives 3rd Generation
BETA-LACTAM ANTIBIOTICS - broad spectrum (E.coli, P.mirabilis, Salmonella) - Activity: more active against G-, less active against
(penicillins, cephalosporins, carbapenems, monobactams)
*inactive: pseudomonas, B. fragilis, penicillinase-producing G+ cocci; variability in activity (Staph, Strep)
Staphylococcus spp. 4th Generation
MoA: bind to penicillin-binding proteins (PBPs) → *combined with B-lactamase inhibitors**: overcome resistance,
↑ spectrum - Activity: broadest spectrum (G+ cocci, G- bacilli,
inhibits transpeptidation → weakens bacterial cell wall
P. aeruginosa, B-lactamase resistant E. coli)
Amoxicillin, Ampicillin* + **clavulanic acid, sulbactam
Effect: bactericidal *poorly absorbed if administered after meal
PK: excreted via urine unchanged Anti-staphylococcal PCNs Cefquinome: evaluated in veterinary medicine
Adv fx: CNS reactions (excitement, seizures), allergic (B-lactamase stable/resistant penicillins) - licensed for use in cattle (also used in pigs)
reactions, predispose to superinfection - stable against B-lactamase by Staph - active against Enterobacteriaceae, staphylococci
- Activity: G+, minimal G- (including MRSA), enterococci
Species consideration: Oxacillin, cloxacillin, dicloxacillin - resistant to B-lactamase
- Slow PCN clearance (long half-life) in REPTILES Synthetic: methicillin, nafcillin 1st Generation 2nd Generation
*infrequent dosing: once q3-5d Anti-pseudomonal PCNs - Cephalexin Cefaclor Cefprozil
(extended-spectrum PCNs) - Cefadroxil Cefoxitin* Cefmetazole
- high renal clearance and metabolic rate in BIRDS - Cephalothin Cefuroxime Cefotetan
*frequent dosing - Activity: G- aerobic, anaerobic (pseudomonas, - Cefazolin Cefonicid Cefamandole
- CIx in GERBILS, HAMSTERS, GUINEA PIG, RABBIT eneterobacteriaceae, proteus, bacteroides sp.) - Cephapirin Ceforanide
Piperacillin, ticarcillin, carbenicillin 3rd Generation 4th Generation
*cause dysbiosis, ATB-associated enteritis, ATB-
Ceftiofur Ceftriaxone - Cefepime
associated clostridial enterotoxemia, overgrowth of
Cefotaxime Cefixime - Cefquinome**
abnormal flora (E.coli, Clostridium sp.) CEPHALOSPORINS Ceftazidime Cefpodoxime
- Procaine Penicillin G (IM, IV) cause excitement in
HORSES -- MoA: bind to PBPs → disrupt cell wall Cefoperazone Cefovecin 5th Generation
Effect: Bactericidal effect Moxalactam - Ceftaroline***
*procaine *ok for P. aeruginosa, obligate anaerobes **ok for veterinary
use Racingmask pain + produce excitation; regulated in
Horses ***new cephalosporin with activity against MRSA
- PK: Distribution – tissues and fluids; rd
poor CNS distribution except some 3 Gen. drugs
Biotransformation – short half-life (given
Microbial resistance to B-lactam antibiotics via
3- 4x/day); minimal hepatic metabolism
B-lactamases* (penicillinase, cephalosporinase)
*inactivate B-lactam ATBs via hydrolysis of B-lactam ring Excretion – renal excretion
(newer: biliary excretion)
Desmopressin TYPES OF FLUID FOR INFUSION
Hypertonic crystalloids
- MoA: release of VWF* CRYSTALLOIDS (3%, 4%, 7% NaCl)
*VWF – mediate plt adhesion in subendothelial spaces - similar with plasma in composition - high Na concentrations → ↑ Na in ECF
→ 1st step in clot formation - Na-based/glucose electrolyte solution → H2O from cells into ECF
- Ix: VON of
- replacement WILLEBRAND’S
lost fluids DISEASE
- Ix: hypovolemic shock
Isotonic crystalloids *cause movement of fluid into intravascular space → tx
Protamine sulfate 0.9% NaCl/isotonic saline/NSS/physiologic saline of shock, reduction of edema
- MoA: strongly basic protein → combines solution - Adv fx: phlebitis, tissue irritation, rehemorrhage
with acidic heparin → stable salt that - Ix: hyponatremia, conditions that require in traumatic shock, electrolyte
prevents anti-coagulant activity of expansion of plasma volume (e.g. imbalances;
heparin shock), bathe tissues during surgery *hypotension, bronchoconstriction, and bradycardia with
- Ix: heparin-induced too fast administration
- CIx: heart failure (due to Na content)
hemorrhage, BRACKENFERN
POISONING Lactated Ringer’s Solution COLLOIDS
- Given slow IV - Salt (Na, K, Cl, Ca) + 28mEq lactate + electrolytes aka Plasma Expanders
ANTI-HEMOSTATIC AGENTS/ANTICOAGULANTS -MoA: large molecules → ↑ blood oncotic pressure
- fluid of choice in many diseases
- interfere with blood clot mechanism - liver: lactate → bicarbonate* →
Systemic Anticoagulants *buffer in acidotic situations (e.g. severe dehydration) fluid to intravascular space
Heparin - CIx: liver disease, cancer, hypercalcemia, - Ix: hypovolemic shock, severe chronic
- MoA: activate antithrombin III → inactivate blood transfusions (Ca – clot blood) disease with hypovolemia, hypoproteinemia
thrombin
- Ix: anticoagulant for BLOOD TRANSFUSION, Normosol® Natural colloids: plasma, albumin, whole blood
PULMOnary EMBOLISM, venous - all purpose replacement fluid Synthetic colloids: dextrans, hydroxylethyl starch
THROMBOSIS (e.g. DIC) - less NaCl, more K & Mg, No Ca (compared to LRS) (hetastarch/HES), oxyglobin (purified solution of bovine Hg)
- (+) acetate and gluconate – dual buffering
Vitamin K antagonists (warfarin, coumarin derivatives) - Ix: px with liver disease Signs of overhydration:
- toxicological importance - compatible for blood transfusion Nasal discharge, chemosis, restlessness, cough
- MoA: inhibit utilization of Vit K & dyspnea, exophthalmos, diarrhea, vomiting
- Ix: long term tx for THROMBOEMBOLISMS Plasmalyte A ®
In vitro Anticoagulants - balanced replacement solution
Na oxalate, Na citrate, Disodium - less Cl, more Mg, no Ca (compared to LRS)
EDTA - (+) acetate and lactate – buffer components
- MoA: chelates Ca from clotting process - irritating to tissues (cannot be given SQ)
*Na citrate – anticoagulant for blood collection for transfusion Hypotonic crystalloids
Dextrose 5% in water (D5W)
Heparin Na
- non-balanced; 50g/L dextrose in water
- anticoagulant for blood sample collection
- equivalent to administering pure water*
Antithrombotics *dextrose immediately metabolized
Aspirin - Ix: hypernatremia, CHO source, fluid
- MoA: cause irreversible, long lasting prevention supplement in px that cannot tolerate Na
of plt agg → prolonged bleeding time - CIx: not given SQ*; not for maintenance
*activity observed even at low doses
*no electrolytes, intracellular, IV electrolytes drawn to SC
- Ix: THROMBOEMBOLISM associated with
heartworm (canine px undergoing adulticide Dextrose 2.5% with 0.45% saline
tx – however, no longer recommended), - Ix: px at risk if given too much Na, those
Feline cardiomyopathies w potential fluid retention
- Adv fx: GIT bleeding, vomiting
- use with caution in CATS Half strength LRS with 2.5% dextrose
- slightly more balanced
DIURETICS K-sparing diuretics HEMOSTATIC DRUGS/COAGULANTS
- Leads to reduction of preload, ascites, pulmo edema - may be used with thiazides/other potent
*requires a functional kidney
diuretics; avert excess K loss LOCAL HEMOSTATIC AGENTS
- Ix: conditions characterized by fluid retention - Ix: persistent capillary bleeding
(heart failure, inflammation or trauma, Spirinolactone - requires intact blood coagulation mechanism
hypoproteinemia, renal failure, high blood - aka aldosterone antagonist - usually absorbable
pressure - MoA: aldosterone antagonist in the collecting duct
*most commonly used in VetMed: Natriuretic agents (thiazides), K-
Clotting factors
- usually combined with loop diuretic/thiazide
sparing diuretics (spironolactone), loop diuretics (furosemide) Topical thromboplastin
- MoA: thromboplastin → thrombin; ↑ coagulation
triamterene, amiloride
Cardiovascular diuretics (xanthine derivatives) - Ix: surgery
- mild diuretics, acts on the collecting duct
- MoA: ↑ renal blood flow → ↑ rate of urine prod’n - not associated with aldosterone
- mild diuretic potency; CNS, cardiac stimul’n, BD Thrombin
- MoA: reduce entry of Na in distal tubule
- MoA: fibrinogen → fibrin
- Diuretic effect usually enhanced by simultaneous Loop diuretics
administration of another diuretic (e.g. thiazide) - Ix: bleeding from parenchymatous
- Site: Loop of Henle
Theophylline, aminophylline tissue, Cancellous bone, dental
- rapid onset
Osmotic diuretics socket, laryngeal/nasal surgery
Adv fx: hypokalemia, hyponatremia, dehydration,
- hypertonic/isotonic solutions, neither metabolized - white sterile powder of bovine origin
weakness, shock, OTOTOXICITY (avoid
nor reabsorbed - must NOT be injected (else, intravascular clotting)
with aminoglycosides)
- MoA: osmotically attracts H2O → ↑ urine volume bumetanide, ethacrynic acid, muzolimine
Fibrin foam
Furosemide/frusemide
- absorbable gelatin applied directly
Mannitol - MoA: inhibit Na, Cl reabsorption (ascending LoH) - Ix: capillary/venous bleeding
- Ix: cerebral edema, renal shutdown (e.g. acute - extremely potent Artificial matrices
renal ischemia, acute changes in renal - Ix: edema
Absorbable gelatin sponge
tubular permeability), ARF
- sterile, water-insoluble, gelatin-based; absorbable
- CIx: Heart failure*, cardiovascular shock** UROLITH TREATMENT
*may worsen pulmonary edema - Ix: capillary, venous bleeding
**excessive mannitol admn → severe hypovolemia
Acidifier Dissolve struvite Methionine
Natriuretic Agents Ammonium Cl Oxidized cellulose
- drugs that promote natriuresis, not reabsorb Na Alkalinizer Ca oxalate, cystine, Potassium - surgical gauze
ammonium urate citrate - rxn of Hg and cellulosic acid → gummy matrix
Thiazides Xanthine ↓ uric acid → Allopurinol - Ix: temporary packing in bleeding points
- MoA: inhibit Na, Cl reabsorption in early oxidase ↓ ammonium urate (interferes with bone regeneration,
distal tubule inhibitor urolith formation epithelialization)
(preventive)
- Ix: edema Microcrystalline collagen
- Adv fx: hypokalemic (may be given with K- - quickly adheres to wet surfaces
sparing diuretics), hypomagnesia, URINARY INCONTINENCE - Ix: surface hemostatic agent during surgery
Bladder hypercalcemia,Cholinergic agonist(inhibits
hyperglycemia Vitamin SYSTEMIC
K1 (phytonadione)
HEMOSTATIC AGENTS
hypocontractility (Bethanechol)
insulin secretion) - co-factor for factors II, VII, IX, X
Bladder Anticholinergic
Chlorthiazide, hydrochlorthiazide, agent
bendrofluazide - Ix: Vit K deficiency*, ingestion of Vit K antagonists**
hypercontractility (Propantheline, *prolonged adm’n of sulfonamides
**anticoagulant rodenticides: blocks epoxide reductase
butylhyoscine)
Carbonic anhydrase inhibitors 1st gen (warfarin, indanedione), 2nd gen (bromadiolone,
Urethral incompetence a-adrenergic
- MoA: inhibit carbonic anhydrase agonist
in renal brodifacoum – more toxic and persistent in the liver)
(phenylpropanolamine)
tubular cells → reduces availability of H - Adv fx: anaphylaxis, bleeding from injection site
Urethral hyperreflexia
for exchange with a-adrenergic
Na → less Na blocker - PK: effects 6-12 hrs
reabsorbed (phenoxybenzamine)
- Ix: systemic acidosis, txskeletal muscle relaxant
of GLAUCOMA
(dantrolene)methazolide,
Acetazolamide*, dichlorphenamide,
ACE INHIBITORSANTIARRHYTHMIC DRUGS CLASS II
- MoA: block Angiotensin II production → VD, ↓BP (Beta-adrenergic blockers)
- other effects: ↓ capillary pressure, edema CLASS I MoA: block B-adrenergic receptors → ↓ myocardial
formation; ↑ tissue perfusion (Local anesthetic agents – Membrane stabilizers) requirement for oxygen
- Ix: treatment of hypertension from CHF MoA: block fast Na channels in myocardial cell Ix: supraventricular, ventricular tachyarrhythmias
- Adv fx: renal failure membrane → impede depolarization Propanolol, oxyprenolol, alprenolol
Ix: ventricular tachycardia,
Captopril, enalapril atrial tachycardia,
maleate*, benazepril PVC Propranolol
*active form: enalaprat CLASS IA - non-selective beta-blocker
- MoA: ↓ excitability, prolong refractory period → - of value in conditions where the heart has
VASODILATORS ↓ rate of depolarization been sensitized to the actions of
- MoA: peripheral VD → ↓ workload (↓ LV
catecholamines (eg halogenated anesthetics,
afterload), smooth mm relaxation in vv. Quinidine sulfate digitalis overdose, myocardial infarcts
and aa. - horse (oral route), large dogs
*venodilators: ↑ venous capacitance, ↓ edema
- Ix: hypertrophic cardiomyopathy,
- Ix: atrial arrhythmia ventricular arrhythmias
*arterial dilators: ↓ systemic arteriolar resistance
- Adv fx: cardiac depression, ↓ cardiac output, - Adv fx: bradycardia, lethargy, depression
Prazosin: block a1 ad. receptor → vv and aa dilator hypotension, vomiting, diarrhea, CNS effects
Hydralazine: arteriolar dilator CLASS III
Nitrovasodilators (nitroprusside, nitroglycerin): Procainamide
(Agents that prolong AP duration)
vv and aa dilator - less GIT effects
MoA: inhibits NE release → lengthen time bet AP
Ca-channel blockers - Ix: intravenous control of atrial arrhythmia
(↑ AP duration, refractory pd in purkinje fibers,
- MoA: block Ca influx, inhibit Ca release ventricular myocardium)
Disopyramide
from SR → ↓ myocardial contractility, Ix: emergency tx for ventricular tachycardia, fibrillation
CLASS IB
VD, slow AV impulse conduction
- MoA: block Na influx into cell, Adv fx: vomiting, hypotension
- Ix: HF, HCM, hypertension (cats),
prevents depolarization Bretylium, amiodarone, sotalol
circulatory shock & trauma
Amlodipine, diltiazem, verapamil
Sildenafil (Viagra) Lidocaine (without epinephrine) CLASS IV
- MoA: PDE V* inhibitor → VD - with local anesthetic activity, IV (Calcium entry blockers, Ca channel blockers/antagonist)
*high conc’n in pulmonary hypertension - Ix: ventricular tachycardia, PVCs MoA: block Ca entry into myocardial cells → slows
Carvedilol down conduction rate, frequency via AV node
Tocainide Ix: supraventricular tachyarrhythmias
- also an anti-epileptic drug, PO Verapamil
DIURETICS
- Ix: ventricular arrhythmias (ventricular - PO, IV
- Ix: Relief of pulmonary congestion and tachycardia, PVCs)
peripheral edema - Ix: supraventricular tachycardia, atrial flutter
- Adv fx: ataxia, vomiting, hypotension
nifedipine, diltiazem
Mexiletine - PO
- PO - Ix: atrial fibrillation, supraventricular tachycardia
- Ix: ventricular arrhythmias (ventricular - Adv fx: edema, hypotension
tachycardia, PVCs)
- Adv fx: vomiting, unsteadiness
Phenytoin
CLASS IC
- slow conduction, little effect on AP duration, rarely
used
Encainide, felacainide
EXPECTORANTS
Centrally-acting antitussives: Non-narcotic
- MoA: dilution and liquefaction of secretions to ↑ flow
- Ix: non-productive cough
aids in removal of secretion by ciliary - non-addicting
action/cough Dextromethorphan (opiate derivative), butorphanol
- Ix: presence of productive cough tartrate (opiate) Digitalis glycosides
- Adv fx: mild drowsiness, nausea - Source: derived from foxglove plant
Ethylenediamine dihydroiodide (EDDI) BRONCHODILATORS - MoA: inhibit Na-K ATPase → ↑ intracellular
- MoA: vagal-mediated reflex action on gastric B2-receptor agonists Na; Ca accumulation in myocardium →
mucosa → stimulate bronchial mucus - functional antagonists of airway stronger contraction
secretions obstruction regardless of stimulus - Fx: ↓ BP, small direct diuretic effect
- Ix: mild resp. disease (horse, cattle) - MoA: direct stimulation (B2 adrenergic receptors) - PK: SI – main site of absorption
- Adv fx: tachycardia, hypertension Enterohepatic recycling, urine
Hypertonic saline excretion
- aerosol form Selective: terbutaline, albuterol (salbutamol), *Digoxin: 25% plasma protein bound
- MoA: attracts fluid via osmosis metaproterenol, pirbuterol, clenbuterol, salmeterol - Ix: CHF, atrial arrhythmias (atrial fibrillation)
Non-selective: epinephrine, pseudoephedrine, - CIx: circulatory shock, renal failure, hepatic
Guaifenesin (glyceryl guaiacolate) isoproterenol failure, ventricular tachycardia, heart block,
- MoA: irritant action on vagus nerve → ↑ secretion Ractopamine: lipolytic effect (livestock, lean meat) ventricular premature contraction
- more commonly used in horses *leaves low levels of residue in food - Adv fx: cardiac arrhythmia, K-depletion in
Methylxanthines cells, mild GI disturbance (diarrhea,
MUCOLYTICS - MoA: inhibit PDE in smooth mm cells → vomiting, inappetence)
- MoA: breakdown of disulfide bonds → cAMP accumulation → BD, mild cardiac - administered by BSA
stimulation, diuresis - high toxic/therapeutic dose ratio
decrease viscosity of mucus
- Ix: resp and cardiac ds that would benefit - tablet/injectable
Acetylcysteine *large dog breeds require less digitalis/kg BW
- Ix: respiratory ds with tenacious mucus from BD; myocardial stimulation
*recommended BID digoxin dose: 0.22mg/m2
*used for paracetamol/acetaminophen poisoning in cats Theophylline, etamiphylline, camsylate, *10kg dog: 0.011mg digoxin/kg q12h
aminophylline, caffeine, theobromine
DECONGESTANTS Antihistamines Digoxin, digitoxin, ouabain
- MoA: stimulate a-adrenergic receptors in m.m. → - MoA: H1 receptor inverse agonist Bipyridine compounds
- Ix: allergic and resp conditions (HEAVES, - nonglycoside, noncatecholamine inotropic drug
local VC → reduce swelling → ↓ congestion
pneumonia, feline asthma, insect bites) - mild systemic arteriolar dilation
Topical: phenylephrine, oxymetazoline,
Pyrilamine, tripelennamine, diphenhydramine, - MoA: inhibits PDE-3 → ↑ intracellular cAMP →
xylometazoline
Systemic: pseudoephedrine, phenylpropanolamine doxylamine, clemastine, cetirizine, cyproheptadine* ↑ cardiac inotropy, VD
*appetite stimulant
Anticholinergics Amrinone/Inamrinone: short-term inotropic support
ANTITUSSIVES (cough suppressants) - MoA: block Ach receptors w myocardial failure; incompatible with dextrose
- Ix: persistent, unproductive cough that interferes Ipatropium bromide: bronchospasm in RAO
Milrinone: incompatible w furosemide
with rest or causes muscle fatigue and
exhaustion RESPIRATORY STIMULANTS (ANALEPTICS)
- MoA: VD (PDE-3 inhibition),
- CIx: excessive respiratory secretion
positive inotropic (↑ intracellular Ca)
Locally-acting antitussives - MoA: stimulate carotid/aortic chemoreceptors →
- Ix: CHF secondary to DCM, CVD, endocarditis
- MoA: soothes irritated resp. m.m. stimulate respiratory center in medulla →
- PK: bioavailability reduced by food (give
menthol, tincture of benzoin, benzonatate ↑ rate and depth of respiration
1hr before intake)
Centrally-acting antitussives: Narcotic - Ix: RESP DEPRESSION from anesthesia,
- well tolerated with px with heart failure
- Ix: harsh, non-productive cough sedatives, hypnotics; APNEIC
- formulation: hard gelatin capsule
- relatively toxic to cats; addiction in humans NEONATES, preterm animals; TX OF
- Adv fx: sedation, constipation HYPERCAPNIA (hypoxic-ischemic
Pimobendan
Codeine, morphine, hydrocodone (controlled opiates) encephalopathy (foals))
Doxapram DRUGS FOR CONGESTIVE HEART FAILURE
Methylxanthines *alters sensitivity of resp center
POSITIVE INOTROPES
- MoA: ↑ force of myocardial contraction
INODILATORS
Proton Pump Inhibitor LAXATIVES PROKINETICS
- MoA: binds to proton pump at luminal surface Ix: relieve constipation or intestinal impaction, remove - MoA: increase movement of ingesta
of the parietal cell that pumps H ions into toxic materials from GIT, soften stool during (coordinated motility patterns)
gastric lumen → suppression of HCl production rectal/vaginal/uterine prolapse, prevent straining - Ix: intractable vomiting associated with
- Adv fx: constipation, sedation, ileus, pancreatitis, during post-op care, remove gut edema fluid, clean metabolic disorders, gut infections
CNS effect
bowel before x-ray/endoscopy Dopaminergic antagonists
Omeprazole, lansoprazole, pantoprazole,
Osmotic agents Metoclopramide
rabeprazole
- MoA: increase H2O → soften stool, - Ix: gastroesophageal reflux, delayed gastric
Synthetic prostaglandin E1 analog
stimulate stretch receptors for peristalsis emptying, GIT motility disorders (dogs, cats),
Misoprostol
- Adv fx: cramping, GIT stimulation (foal)
- MoA: inhibits HCl secretion from parietal cell
nausea MgOH, Lactulose
into stomach → stimulates gastric mucus
Stimulant (irritant) laxatives Domperidone: regulate GIT motility
secretion
- MoA: irritate GIT mucosa → ↑ peristalsis Serotonergic antagonist
- Ix: NSAID-induced ulceration *seldom used in Vet Medicine Cisapride
- Adv effect: abortion, diarrhea, Emodin, castor oil, bisacodyl (Dulcolax) - MoA: enhance Ach release → motility (esophagus
flatulence, vomiting, abdominal pain Bulk-forming laxatives → colon)
- MoA: indigestible plant material → absorbs - Ix: gastroesophageal reflux, GI stasis (horse,
ANTIDIARRHEALS water, swells → increase bulk & fluidity of dog, cat)
Narcotic analgesics (opiates) intestinal content → peristalsis
- MoA: ↑ segmental contraction - Ix: SAND IMPACTION, constipation DIGESTIVE ENZYMES
↓ intestinal secretion (horses) Psyllium, bran, methylcellulose, - Ix: pancreatic exocrine insufficiency
Enhance intestinal absorption Metamucil - Adv fx: diarrhea, nausea, cramps
- CIx: infectious diarrhea Lubricants Pancrelipase: fat, protein, CHO
- Adv fx: ileus, constipation, sedation, - MoA: soften stool for easier passage digestion
CNS excitement (horse, cats) - Ix: constipation, fecal impaction
Diphenoxylate (Lomotil), loperamide (Imodium)
Anticholinergic drugs (antispasmodics) ANTIBIOTICS
Mineral oil: constipation, COLIC, IMPACTION
- MoA: ↓ intestinal motility & peristalsis Ix: bloody diarrhea, sepsis
(horses)
*may destroy intestinal microflora and allow growth
↓ reduce gastric secretions Petrolatum: HAIRBALLS (cats) of bacterial pathogens
-Ix: relief of pain & tenesmus (large bowel Stool softeners Metronidazole – antibacterial, antiprotozoal
inflammatory disease), relief of spasms in gut - MoA: reduce surface tension → water enters Amoxicillin, clavamox, tylosin
spasms, stress-induced colitis (with cholinergic GI contents
involvement) - Ix: hard dry feces, impaction, digestive
Aminopentamide, hyoscine, propantheline, APPETITE STIMULANTS
upset Docusate Na, Docusate Ca (Enema
clindinium SA)