Most importante drugzz + factzz (B- topiczz 9-30) Flashcards

Question

B11: DIAZEPAM (anticonvulsant)

Answer 1

GROUP: Benzodiazepines MOA: Activation of the benzodiazepine binding site on GABAA, which lead to hyperpolarization of the postsynaptic neuron producing decreased neuronal transmission PK: Highly lipid soluble, good oral absorption, long onset of action IM but fast onset IV and PO or IN, can be given rectally, excretion via kidney, can be re-administrated SE: Alone: Paradoxical excitement, agitation, vocalization, and dysphoria may be seen after IV or IM administration INDICATIONS: Status epilepticus and appetite stimulant. CONTRAINDICATION: - Paradoxical reaction (cat, greyhound) - Aminoglycosides (inhibition of respiration) DOSAGE: Ca: IV: 0.5-2 mg/kg Fe: IV: 0.5-2 mg/kg

Answer 2

GROUP: Benzodiazepines MOA: Amplify inhibitory effects of GABAA, nerve inhibtion by allowing Cl- into cell. PK: Metabolized in liver, can be absorbed intranasally, no first pass effect, shorter and less sedation than diazepam. Water soluble, but becomes lipid soluble in the body SE: Decrease respiratory rate, ataxia, weakness INDICATIONS: Pre-anastethic (w/ ketamine), anti-epileptic (status epilepticus), muscle relaxant CONTRAINDICATION: Food producing animals and new borns (high liver toxicity)

Answer 3

GROUP: Injectable anaesthetics/ anticonvulsants MOA: Decreases the rate of GABA dissociation from its receptors thus increasing the opening of chloride channels PK: Milky white emulsion, fast distribution, quick hepatic metabolism (can be used in liver failure patients), excretion in urine, given IV SE: Cardiac, respiratory and renal impairment, negative inotropic effect--> hypotension, increased ocular pressure--> not good in glaucoma INDICATION: Used in status - epilepticus seizures DOSAGE: Dog/ Cat: - IV 6-8 mg/kg (without premedication) - IV 3-4 mg/kg (with premedication)

Answer 4

GROUP: Barbiturate MOA: GABAa, decrease Ca2+ accumulation --> inhibits the release of stimulatory neurotransmitters PK: Respiratory depression, re-distribution in fat and muscle, accumulation in fat, excreted in urine SE: Respiratory and cardiovascular depression, tissue irritation, liver insufficiency INDICATION: Epilepsy in dogs (long-acting) CONTRAINDICATION: Greyhounds are oversensitive

Answer 5

GROUP: Phentothiazine MOA: Sedation by inhibiting postsynaptic central dopaminergic receptors (alpha 1 receptor) PK: Large Vd, slow elimination, metabolise in liver, excretion in urine, bioavailability: PO-20% SE: Penile prolapse and hypertension in eq, third eyelid prolapse in ca and fe, constipation, and dry mouth, paradoxical reactions INDICATION: Calming, sedation, muscle relaxation, premedication DOSE: Dog: PO: 1-2 mg/kg IM/IV: 0.2-0.3 mg/kg Horse: PO: 0.1-0.4 mg/kg IM/IV: 0.03-0.1 mg/kg

Answer 6

GROUP: Benzodiazepine MOA: Amplify inhibitory effects of GABA, nerve inhibtion by allowing Cl- into cell. PK: Metabolism in liver, more potent than diazepam SE: Alone: Paradoxical excitement, agitation, vocalization, and dysphoria may be seen after IV or IM administration INDICATION: Anxiety and panic attacks

Answer 7

GROUP: Benzodiazepines MOA: Activation of the benzodiazepine binding site on GABAA, which lead to hyperpolarization of the postsynaptic neuron producing decreased neuronal transmission PK: Highly lipid soluble, good oral absorption, long onset of action IM but fast onset IV and PO, excretion via kidney SE: Alone: Paradoxical excitement, agitation, vocalization, and dysphoria may be seen after IV or IM administration INDICATIONS: Epilepsy, anaesthetic induction, muscle relaxants, appetite stimulant in cats, can be used in heart patients IN COMBINATION: Ketamine and etomidate CONTRAINDICATION: - Paradoxical reaction (cat, greyhound) - Aminoglycosides (inhibition of respiration) DOSAGE: Ca: IV: 0.5-2 mg/kg Fe: IV: 0.5-2 mg/kg

Answer 8

GROUP: Tricyclic antidepressant MOA: Inhibit the Serotonin + NA reuptake → anticholinergic, antiadrenergic, and antihistamines. PK: Good oral absorption, high albumin binding, long onset of action, metabolize in liver, excretion in urine SE: - Sedation - Lethargy - Vomiting - Antimuscarinic - Change in Appetite - Urinary Retention INDICATION: -Separation anxiety -Feline urine spraying - Acral lick dermatitis CONTRAINDICATION: Cardiovascular dysfunction, epilepsy

Answer 9

GROUP: Selective serotonin reuptake inhibitor MOA: Selective inhibition of serotonin reuptake PK: Good oral absorption, bound to albumin, metabolize in liver, elimination half-life 7-9 days SE: Occasional vomiting INDICATION: Stereotypes, aggression, depression, feline urine spraying, separation anxiety CONTRAINDICATION: Epilepsy and hepatic impairment

Answer 10

GROUP: A2- antagonist and antidepressant MOA: A2 and H1 antagonism PK: Elimination half life 40hrs in dogs and 10hrs in cats, given PO SE: Vocalization and increased restlessness INDICATION: Antidepressant and anti-emetic agent and apetite stimulation in cats

Answer 11

GROUP: Central muscle relaxant, (Glycerol guaiacolate, Guaiacolglycerol ether) MOA: They have a relative specific depressant action on CNS, causing decreased motor activity or paralysis of voluntary muscles without loss of consciousness PK: Fast onset and elimination of action, large distribution, crosses placenta barrier, excretion in urine, given as infusion SE: Mild, slight decrease of arterial blood pressure, respiratory depression (in large doses) and haemolysis INDICATION: Horses, cattle, sheep – to adjunct anaesthesia, dogs – strychnine poisoning (in pass). They are also used to control certain spasmodic and painful disorders of skeletal (spinal) muscles

Answer 12

GROUP: Aminosteroid, peripheral muscle relaxant MOA: Mechanisms of action are competitive antagonists of NACh. The blockade starts when 70-80% of receptors are antagonised. Complete block at 90% Blocking agents not metabolised at neuromuscular junction PK: Long duration of action, poor absorption from GIT, metabolized in liver, excreted in kidney, SE: Cardiovascular effects and release of histamine INDICATION: Muscle relaxation CONTRAINDICATION: Duration of action increased in patients with renal and hepatic dysfunction.

Answer 13

GROUP: Benzylisoquinoline (Nondepolarizing / Competitive NM Blocking Agent) MOA: Mechanisms of action are competitive antagonists of NACh. The blockade starts when 70-80% of receptors are antagonised. Complete block at 90% Blocking agents not metabolised at neuromuscular junction PK: Intermediate duration, metabolised in plasma (safe in liver and kidney disease), precipitated in alkaline PH SE: Bradycardia INDICATION: Muscle relaxation

Answer 14

GROUP: Succinylcholine chloride (Depolarizing NM blocking drug) MOA: Stimulates the opening of the NACh receptor Depolarisation of the cell membrane Inactivation of voltage-gated Na channels → no further action potentials PK: Rapid onset of action, short lasting block, can be given IM in emergency, terminated in liver SE: Bradycardia, paralysis/weakness, hyperkalaemia, high IOP (dogs, cattle, sheep = sensitive, horses, pigs = less sensitive), increases blood pressure, anaphylaxis, malignant hyperthermia INDICATION: Assist in intubation (?)

Answer 15

GROUP: A2 agonist MOA: Presynaptic binding of α2-adrenergic receptors --> decreased release of norepinephrine PK: Fast absorption, good distribution (crosses barriers, metabolize in liver, excretion in urine, works within few mins iv and 10-15 mins im SE: Emetic in cats and some dogs, penile prolapse in horse INDICATION: Provide sedation, chemical restraint, analgesia, used against hyperglycemia and glaucoma CONTRAINDICATION: Boxers/rottweilers DOSAGE: Dogs and cats: IM, IV, SC; 1-4 mg/kg Cattle: IV, IM: 0.05- 1mg/kg Horse: 0.5-1mg/kg

Answer 16

GROUP: a2 agonist MOA: Presynaptic binding of α2-adrenergic receptors --> decreased release of norepinephrine PK: Fast absorbtion, good distribution, iv: immediately, im: few mins, metabolize in liver, excretion in urine, high bioavailability in catlle (less in eq) SE: Penile prolapse in eq, hypothermia, diuresis INDICATION: Provide sedation, chemical restraint, analgesia, good premedication, used in hyperglycemia IN COMBINATION: With thiopentone, ketamine or opioids CONTRAINDICATION: Food producing animals

Answer 17

GROUP: a2 agonist MOA: Presynaptic binding of α2-adrenergic receptors --> decreased release of norepinephrine PK: Fast absorbtion, good distribution, iv: immediately, im: few mins, metabolize in liver, excretion in urine SE: Vomiting, thermoregulatory issues, constipation, bradychardia INDICATION: Provide sedation, chemical restraint, analgesia, good premedication, used in hyperglycemia IN COMBINATION: With thiopentone, ketamine or opioids CONTRAINDICATION: Food producing animals DOSE: Dog: IM, IV 5-10 μg/kg (pre-anaesthesia) IM, IV 10-20μg/kg (sedation + analgesia) Cat: IM, IV 40 μg/kg (both doses)

Answer 18

GROUP: (Vasodilator and class IV antiarrhythmic) and calcium channel blocker) MOA: Increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. It is a negative inotrope PK: Well absorbed from the GI SE: Rare, but vomiting and anorexia have been observed in cats INDICATION: Hypertension and angina

Answer 19

GROUP: Phosphidiesterase inhibitor MOA: Inhibits the PDE3 enzyme in the heart muscle → accumulation of cAMP → increase in calcium concentration → Positive inotropic effect PK: Given orally, one hour before meals, as feeding decrease its absorption and causes vomiting SE: Very rare, mainly GI related (vomiting and diahrrea) INDICATION: - Prolong survival time in heart failure - Supraventricular tachyarrhytmias CONTRAINDICATION: Outflow obstruction (HCM, stenosis) i.e. must perform an ultrasound before administration

Answer 20

GROUP: Esters (local anaesthetic) MOA: Act by blocking conduction in nerve fibres → without loss of consciousness or a depressed activity of CNS PK: Determine absorption: site of application, dose, vasoconstriction. Duration of action: until concentration falls below critical level due to absorption from site of application. Metabolism hydrolysed by plasma esterase and degraded by hepatic metabolism SE: Allergy, asthmatic seizure, local irritation, confusion, tremor INDICATION: Topical anaesthesia: Numbing the surface of the eye

Answer 21

GROUP: Amide MOA: Block action potential generation by blocking Na+ channels. Act in their cationic form (they must be weak bases), but they must reach their site of action by penetrating the nerve sheath and axonal membrane as unionised species. PK: Rapid onset of action, moderate protein binding, low lipid solubility. SE: Asthmatic seizure, local irritation, confusion, tremor, fall in blood pressure INDICATION: Used to ease pain from skin irritation, rectal painful disease

Answer 22

MOA: Block action potential generation by blocking Na+ channels. Act in their cationic form (they must be weak bases), but they must reach their site of action by penetrating the nerve sheath and axonal membrane as unionised species. PK: High potency, medium onset of action, long-acting, high protein binding, highly lipophilic. SE: Asthmatic seizure, local irritation, confusion, tremor, fall in blood pressure INDICATION: is frequently the drug of choice in situations that require use of a long-acting agent (surgery or labor)

Answer 23

GROUP: Amide MOA: Block action potential generation by blocking Na+ channels. Act in their cationic form (they must be weak bases), but they must reach their site of action by penetrating the nerve sheath and axonal membrane as unionised species. PK: Long-acting, almost as high efficacy and potency as bupivacaine, but is safer to use SE: Spinal cord injury, local irritation, confusion, tremor, fall in blood pressure INDICATION: Spinal block (epidural), surgery of perineal region, anal or peri-anal region, obstetric operations, urology

Answer 24

GROUP: Amide MOA: Block action potential generation by blocking Na+ channels. Act in their cationic form (they must be weak bases), but they must reach their site of action by penetrating the nerve sheath and axonal membrane as unionised species. PK: Rapid onset of action, moderate protein binding, low lipid solubility, penetrates BBB. Advantage → no negative inotropic effect i.e. can be given in heart failure. SE: CNS effects (excitation, tremors and convulsion. This can be treated with diazepam) INDICATION: Ventricular arrythmia CONTRAINDICATION: Cats are sensitive, so use lower dosage! NOTE: Potassium supplementation is necessary (hypokalemia)

Answer 25

GROUP: 1st gen B- antagonist (non-selective), Beta blocker. MOA: Blocking B- receptors, causing vasoconstriction. Hypotensive → 1st generation, group II antiarrhythmics PK: Well absorbed from GI tract, it is lipophilic, has large Vd, low bioavailability SE: Cough, difficulty breathing (bronchoconstriction) INDICATION: Decreases blood pressure, stimulate the heart CONTRAINDICATION: Asthma patients

Answer 26

GROUP: Sodium channel blocker MOA: PK: High bioavailability, SE: Rare(??) INDICATION: It is used in cardiomyopathy as well as ventricular arrhythmia It is combined with beta blockers frequently.

Answer 27

GROUP: Specific B-antagonist (Beta blocker) MOA: Blocking B1- receptors, causing vasoconstriction. Belongs to 2nd generation Group II antiarrhythmics. PK: Local anaesthetic activity, large Vd, metabolize in liver, short half-life in small animals SE: Bradychardia, dizziness INDICATION: Slows down heart rate -> Hypotensive

Answer 28

GROUP: (Vasodilator and class IV antiarrhythmic) and calcium channel blocker) MOA: Increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. It is a negative inotrope PK: Well absorbed from the GI SE: Rare, but vomiting and anorexia have been observed in cats INDICATION: Hypertension and angina

Answer 29

GROUP: Cardiotonic (from the digitalis lanata plant) MOA: They inhibit the Na+/K+ ATPase enzyme which is responsible for Na+ efflux and K+ influx -> increased contractility of the heart -> Positive inotropic effect PK: - Positive inotropic effect → improves the renal blood flow → increases water and Na+ excretion, given orally, excretion via kidney SE: Cardiac arrythmias and bradycardia, hypokalemia and extracardial signs are GI-signs like vomiting. It has a narrow therapeutic index INDICATION: Prolong survival time in heart failure, supraventricular tachyarrhytmias (it increases contractility) CONTRAINDICATION: Should not be given with NSAIDs, glucocorticoids or Furosemide as they will compete for the protein albumin and it should not be used in patients with renal failure ANTIDOTE: Digibind

Answer 30

GROUP: Osmotic laxative MOA: They absorb water from the environment of the GI tract and from the body system (water retention). PK: Quick acting, given orally SE: Dehydration INDCATION: Against constipation CONTRAINDICATION: They require rehydration via infusion before these are given

Answer 31

GROUP: Sugar alcohol (and very important laxative) MOA: In the colon, this drug is activated and decomposed by the bacteria to form smaller chain acids e.g. lactic acid, acetic acid, propionic acid, butyric acid etc. These smaller chain acids are what are responsible for the action of absorbing water to cause osmotic diarrhoea. PK: Bad penetration through membrane, given rectally or PO SE: Convulsions INDICATION: Hepatic encephalopathy and against constipation

Answer 32

GROUP: Coating agent MOA: It is given orally to soften and cover the faeces to make it slippery PK: Given PO, is very lipophilic SE: Long-term use (more than 1 week) can cause vitamin deficiency, a small amount can also be absorbed to form irreversible granulomas in the intestinal wall and liver, leading to stomach pain in both animals and humans INDICATION: Against constipation (It is given orally to soften and cover the faeces to make it slippery)

Answer 33

GROUP: Adsorbent MOA: It can bind the bacterial endo- and entero-toxins PK: Very potent, used alone or in combination SE:?? INDICATION: This is frequently used, especially in cases of poisoning where we have toxins in the body

Answer 34

GROUP: Magnesium-aluminium silicate (adsorbent) MOA: Its property is that it can disinfect the GI tract i.e. it has an antimicrobial as well as an antidiarrhoeal effect. PK: Can be used alone.

Answer 35

Group: Bismuth-subsalicylate (adstringents) MOA: These also bind and precipitate the damaged proteins to form a layer to coat the GI tract where it was damaged i.e. they form a protective layer. Not only the damaged proteins but also the toxin proteins can be bound and coagulated i.e. they can also act on other types of diarrhoea as well. PK: More potent than adsorbents, and can be used in combination with them SE: Can make faeces black INDICATION: These drugs cause vasoconstriction and decrease the secretion of the GI tract i.e. help with diarrhoea. They also have an anti-inflammatory effect CONTRAINDICATION: Cats (they are sensitive to salicyclic acid)

Answer 36

GROUP: Tropane alkaloid (parasympatholytic) MOA: M-ACh antagonist. Interacts with muscarinic receptors of effector cells and, by occupying these sites, prevent ACh from binding to the receptor. PK: Well absorbed, crosses BBB, distributed in tissues, metabolize in liver and excretion via urine. Narrow TI (be careful with dosaging) SE: Excessive salivation and vomiting, increase in IOP, decrease tear production INDICATION: Cyclopegia, causes mydriasis, synechiae, iritis (inflammation of vascular membrane of the eye) CONTRAINDICATION: Patients with glaucoma or KCS (?) DOSE: Dog: IM, IV 0.02 mg/kg (OP poisoning 0.2-0.5 mg/kg IV 1/4, SC 3/4)

Answer 37

GROUP: Quaternary ammonium compound (parasympatholytic) MOA: Interacts with muscarinic receptors of effector cells and, by occupying these sites, prevent ACh from binding to the receptor. PK: Longer duration of action than atropine, safer to use, excretion in urine (I think) SE: Constipation, hypothermia, cough INDICATION: Pre-medication (decrease salivation) CONTRAINDICATION: Horses with colic

Answer 38

GROUP: Atropine derivative (M-ach antagonist and parasympatholytic) MOA: Non‐selectively blocking muscarinic receptors to cause mydriasis and cycloplegia PK: Rapid onset, short duration of action. SE: Confusion, tachycardia, unsteadiness INDICATION: Used in eye examinations

Answer 39

GROUP: M- ACh antagonist (Parasympatholyitc) MOA: Interacts with muscarinic receptors of effector cells and, by occupying these sites, prevent ACh from binding to the receptor. PK: Short half-life. SE: Increase in heart-rate INDICATION: Antispasmodic - used in horses with colic CONTRAINDICATION: Horses with ileus

Answer 40

GROUP: Benzodiazepines MOA: Activation of the benzodiazepine binding site on GABAA, which lead to hyperpolarization of the postsynaptic neuron producing decreased neuronal transmission PK: Highly lipid soluble, good oral absorption, long onset of action IM but fast onset IV, excretion via kidney, can be re-administrated SE: Alone: Paradoxical excitement, agitation, vocalization, and dysphoria may be seen after IV or IM administration INDICATIONS: Status epilepticus and good appetite stimulant in cats. CONTRAINDICATION: - Paradoxical reaction (cat, greyhound) - Aminoglycosides (inhibition of respiration) AND obese cats DOSAGE: Ca: IV: 0.5-2 mg/kg Fe: IV: 0.5-2 mg/kg

Answer 41

GROUP: Serotonin antagonist and modest antagonist for histamine MOA: Produce some benefit against smooth muscle constriction, vasodilation, increased vascular permeability, and inflammatory cell influx PK: Given orally, can penetrate BBB SE: CNS clinical signs (depression agressivity) INDICATION: Allergic bronchitis, RAO, and Feline asthma AND as appetite stimulant in both cats and dogs.

Answer 42

GROUP: A2- antagonist and antidepressant MOA: A2 and H1 antagonism. Most frequently used appetite stimulant PK: Elimination half life 40hrs in dogs and 10hrs in cats, given PO SE: Vocalization, depression, aggressivity, excitation, tremors INDICATION: Antidepressant and anti-emetic agent, and appetite stimulation in cats

Answer 43

GROUP: Peptide hormone MOA: Biosynthesis: Preproinsulin (ER) → Proinsulin (golgi complex) → Insulin (storage in secretory granules. Complex with zinc). Action: PK: - Regular insulin: half-life is 5 mins (insulinase). - Regular Crystalline Zinc Insulin: Rapid onset of action, short duration, given SC (and IV). - Isophane insulin: Intermediate acting because it contains protamine → protein which slows down the absorption of insulin. SE (of Protamine Zinc Insulin) : Allergic reaction, acute hypoglycemia: excessive insulin dose, inadequate food intake, Somogyi rebound effect: hypoglycemia induced hyperglycemia. Due to the compensatory release of insulin antagonists → glucagon, catecholamines. INDICATIONS: → DM in dogs and cats → Ketosis and fatty liver in cattle which are not responsive to glucose or GC therapy alone. Regular Crystalline Zinc Insulin: → rapidly resolve diabetic ketoacidosis → not for maintenance of stable blood glucose level CONTRAINDICATION: PZI is not used in cats

Answer 44

GROUP: Protein hormone (insulin antagonist) MOA: Created in pancreas (alfa cells in islets of Langerhans), it helps increasing blood sugar. Glucagon triggers the liver to convert stored glucose (glycogen) into a usable form and then release it into the bloodstream. This process is called glycogenolysis SE: High blood sugar INDICATION: Diabetes mellitus, type I

Answer 45

(Cannot find anything in PPt's??)

Answer 46

GROUP: Gestagen MOA: 1st generation "strong" gestagen. Induce and synchronise ovulation in heifers and cows (CRESTAR implant) IN COMBINATION: W/ oestradiol INDICATION: Induce and synchronise ovulation in large animals

Answer 47

GROUP: Gestagen MOA: 1st generation "strong" gestagen. Induce and synchronise ovulation in mares and sows INDICATION: Induce and synchronise ovulation in large animals NB!: Absorbed in milk, use with care

Answer 48

GROUP: 2nd gen weak gestagen MOA: Antigonadotrophic effect (cats and dogs) In females: To prevent and suppress oestrus and ovulation in companion animals. In males: Anal adenoma, prostate hypertrophy, benign tumour, increased sexual activity, strange behaviour

Answer 49

GROUP: 2nd gen weak gestagen MOA: Antigonadotrophic effect (cats and dogs) In females: To prevent and suppress oestrus and ovulation in companion animals. In males: Anal adenoma, prostate hypertrophy, benign tumour, increased sexual activity, strange behaviour

Answer 50

GROUP: Antiprogestogen MOA/PK/INDICATION: Used to terminate pregnancy (abortion), given SC

Answer 51

GROUP: Estrogen MOA: They are produced by the granulosa cells of the ovarian follicle, CL., adrenal cortex, testicles, placenta (large quantity in late pregnancy). PK: Can be absorbed through the skin, mucous membrane, GI tract (some hepatic inactivation), SC, IM long acting esters Metabolism in liver → elimination primarily in urine EFFECTS: Development of female sex organs, development and maintenance of secondary female sex characteristics, release of GnRH, slight anabolic effect, fat distribution. SE: Mainly according to prolonged use or administration to large doses: - In cow: postparturient straining with prolapse of vagina, uterus - In dog: anaemia, endometritis - ovarian suppression and hypoplasia → ovarian cysts - feminisation in the male - it should not be given to animals with mammary tumours, and during pregnancy INDICATION: Females: Treatment of uterine infections, stop lactation in bitches and cats, treat cattle having persistent CL Males: Anal adenoma, prostate hypertrophy, benign tumour

Answer 52

GROUP: Gonadotropin-Releasing Hormone MOA: GnRH stimulates the synthesis and release of gonadotropins by binding to the GnRH receptor, a G protein-coupled receptor linked to the IP3-Ca2+ signal transduction pathway. If given continuous: desensitisation/down-regulation of GnRH receptors in pituitary gland → suppression of gonadotropins, basis of medical castration. Effect on FSH/LH of animal: depends on the dose and route of administration, and the endocrine status of the animal. PK: Short half-life (2-4 min), intermittent release, SC, IM (equine IV), SE: Hyperthermia, fever and luteal body cysts INDICATION: → Follicular cysts in cattle → Infertility in cattle → Decreased pregnancy rates in cattle → Induce ovulation in mares, pigs, and rabbits → Facilitate stripping and to induce mortality due to egg binding in rainbow trout CONTRAINDICATION: Pregnancy (embryo transfer) and in starved, cachexia animals

Answer 53

GROUP: Gonadotropin-Releasing Hormone analogue MOA: GnRH stimulates the synthesis and release of gonadotropins by binding to the GnRH receptor, a G protein-coupled receptor linked to the IP3-Ca2+ signal transduction pathway. If given continuous: desensitisation/down-regulation of GnRH receptors in pituitary gland → suppression of gonadotropins, basis of medical castration. Effect on FSH/LH of animal: depends on the dose and route of administration, and the endocrine status of the animal. PK: Short half-life (2-4 min), intermittent release, SC, IM (equine IV), SE: Hyperthermia, fever and luteal body cysts INDICATION: Infertility therapy: Induce ovulation in cattle and horses Pulse dosing to induce estrus in dogs and cats Increase fertility rate in sows and fur-producing farmed animals

Answer 54

GROUP: Gonadotropin-Releasing Hormone analogue MOA: GnRH stimulates the synthesis and release of gonadotropins by binding to the GnRH receptor, a G protein-coupled receptor linked to the IP3-Ca2+ signal transduction pathway. If given continuous: desensitisation/down-regulation of GnRH receptors in pituitary gland → suppression of gonadotropins, basis of medical castration. Effect on FSH/LH of animal: depends on the dose and route of administration, and the endocrine status of the animal. PK: Short half-life (2-4 min), intermittent release, SC, IM (equine IV), SE: Hyperthermia, fever and luteal body cysts INDICATION: Cystic ovaries therapy in cattle: Therapy → GnRH analogues mimic the effect of LH surge and causes ovulation of follicular cyst. Also used in ferrets to terminate estrus

Answer 55

GROUP: Gonadotropin-Releasing Hormone analogue (superagonist) MOA: Stimulate the synthesis and secretion of FSH and LH by interacting with GnRH receptors on the pituitary gonadotropes. PK: SC implant in horses and dogs or injection. Long-acting SE: ?? INDICATION: Indications: → Chemical castration in males → Contraceptive in females → SC implant → 1 year duration of action

Answer 56

GROUP: Gonadotropin MOA: Large glycoprotein, secreted from the endometrial cups of pregnant mares in early pregnancy in order to maintain a luteotrophic (CL stimulatory) effect upon the primary and secondary CL in the mare PK: Long half-life (2-5 days) SE: Anaphylactic reaction INDICATION: → Advance onset of follicular growth and ovulation → Alone or after pre-treatment of progesterones in: cow, goat, ewe → In combination with hCG and estrogen in: sow, ancestry bitches → Superovulation: increase litter size, embryo transfer → Stimulates spermatogenesis and libido CONTRAINDICATION: Pregnancy

Answer 57

GROUP: Human Chorionic Gonadotropin MOA: Is produced only in primates and is synthesized by syncytiotrophoblast cells of the placenta. PK: Half life is 12-24hrs SE: Anaphylactic reaction INDICATION: → Supplement/replace LH in ovulation failure/delay → Oestrus synchronization → Ovulation in mare at time of breeding → Nymphomania due to cystic ovaries (induce luteinizing and then ovulation) → Ovarian stimulation → Cryptorchidism (males) CONTRAINDICATION: Pregnancy

Answer 58

GROUP: Peptide hormones MOA: Binding to receptors → resting potential is changed → Ca-channels are opened → Ca2+ increase → contraction + prostaglandin release PK: Release is controlled by adrenergic and cholinergic pathway, opioid peptides , oestrogen (+ receptor modification) and is stimulated by mechanical stimuli on teat and genital tract. Given IV/SC/IM, fast metabolism, no oral bioavailability SE: GI – Cardio-vascular sys., swelling at inj. site INDICATION: Uterine inertia, during delivery in all species, retention of eggs, after parturition, mastitis, after C-section and uterine prolapse

Answer 59

GROUP: Ergot alkaloid (?) (dopamine agonist) MOA: Acts on the dopamine receptors, creating continous crontractions of uterus and peripheral constriction of vessels PK: Given PO SE: Nausea, vomiting, constipation INDICATION: Pseudopregnancy, abortion (off-label) and synchronization

Answer 60

GROUP: Hypoadrenocorticism (Addison's disease) MOA: Fludrocortisone binding to mineralocorticoid receptors causes alterations to DNA transcription and translation of proteins that result in an increased density of sodium channels on the apical side of renal tubule cells and an increased density of Na+-K+-ATPase on the basolateral side PK: Given PO SE: Hypokalaemia, hypernatraemia, water retention, muscle weakness, hypertension (?) INDICATION: Addison's disease

Answer 61

GROUP: Hyperadrenocorticism (Cushing's syndrome) and antifungal agent MOA: Ketoconazole interacts with 14-α-sterol demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability PK: Acidic environment --> Becomes soluble in water, high plasma binding, metabolised and eliminatied in liver SE: If overdose; Liver injury, anorexia, fatigue, nausea and jaundice INDICATION: Cushing's syndrome

Answer 62

GROUP: Hyperadrenocorticism (Cushing's disease) MOA: Produces suppression of the adrenal cortex by inhibiting enzymatic conversion of steroids by 3-beta-hydroxysteroid dehydrogenase--> blocking synthesis of adrenal steroids PK: ?? SE: Lethargy, weakness, vomiting, acute pancreatitis INDICATION: Cushing's disease

Answer 63

GROUP: Hypothryroidism drugs MOA: Acts as a replacement in deficiency syndromes such as hypothyroidism. T4 is the major hormone secreted from the thyroid gland and is chemically identical to the naturally secreted T4: it increases metabolic rate, decreases thyroid-stimulating hormone (TSH) production from the anterior lobe of the pituitary gland, and, in peripheral tissues, is converted to T3. PK: Given PO, low absorption in cats, but higher in dogs, Tmax is 1-5 hours in dogs, and elimination half-life is 7.5 hours in dogs, elimaination through kidneys SE: Weight loss, increased appetite, palpitations, nervousness, diarrhea, abdominal cramps, sweating, tachycardia INDICATION: Hypothyroidism

Answer 64

GROUP: Hyperthyroidism MOA: Methimazole's primary mechanism of action appears to be interference in an early step in thyroid hormone synthesis involving thyroid peroxidase (TPO), however the exact method through which methimazole inhibits this step is unclear. PK: Rapid oral absorption, no protein binding, rapidly metabolized in liver SE: If overdosed; GI problems, headache, joint pain and edema INDICATION: Hyperthyroidism

Answer 65

GROUP: Peptide hormones (uterus stimulant) MOA: Binding to receptors → resting potential is changed → Ca-channels are opened → Ca2+ increase → contraction + prostaglandin release PK: Release is controlled by adrenergic and cholinergic pathway, opioid peptides , oestrogen (+ receptor modification) and is stimulated by mechanical stimuli on teat and genital tract. Given IV/SC/IM, fast metabolism, no oral bioavailability SE: GI – Cardio-vascular sys., swelling at inj. site INDICATION: Uterine inertia, during delivery in all species, retention of eggs, after parturition, mastitis, after C-section and uterine prolapse

Answer 66

GROUP: Prostaglandin (synthetic) analogue and uterine stimulant MOA: Local hormones -> produced by the endometrium. It is released in late diestrus and near term in all pregnant animals. It is released near term in all pregnant animals. PGF2α mediates a decrease in circulating progesterone via luteolysis (corpus luteum regression) at the end of the cycle and pregnancy. PK: Onset is approx 2-5 days and it should not be given IV but rather IM(?) SE: Colic disorders, nausea, vomiting, diarrhoea, bronchoconstriction, abortion INDICATION: Used for estrous synchronization, – to induce parturition (sows, mares, cows with glucocorticoid) – for abortion – for treatment of pyometra They cause premature luteolysis, thus decreasing estrous cycle length and thereby hastening the onset of estrus CONTRAINDICATION: Pregnant animals

Answer 67

GROUP: Prostaglandins and uterine stimulant MOA: Local hormones -> produced by the endometrium. It is released in late diestrus and near term in all pregnant animals. It is released near term in all pregnant animals. PGF2α mediates a decrease in circulating progesterone via luteolysis (corpus luteum regression) at the end of the cycle and pregnancy PK: Highest potency, it works 2-5 days after cycle, more resistant to metabolism than dinoprost SE: Abortion, diarrhea, abdominal discomfort, bronchoconstriction, and increase in blood pressure. INDICATION: Used for estrous synchronization, – to induce parturition (sows, mares, cows with glucocorticoid) – for abortion – for treatment of pyometra They cause premature luteolysis, thus decreasing estrous cycle length and thereby hastening the onset of estrus CONTRAINDICATION: Pregnant animals

Answer 68

GROUP: Ergot alkaloid (?) (dopamine agonist) and uterine stimulant MOA: Acts on the dopamine receptors, creating continous crontractions of uterus and peripheral constriction of vessels PK: Given PO SE: Nausea, vomiting, constipation INDICATION: Pseudopregnancy, abortion (off-label) and synchronization,

Answer 69

GROUP: Bronchodilator, β-adrenoceptor agonist and selective sympathomimetic (uterus relaxant) MOA: Agonism of the beta(2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles and uterus PK: Given PO SE: - Tachycardia, tremors and a decreased uterine contraction → decreased by inhalation INDICATION: Used primarily for the treatment of recurrent airway obstruction (RAO) in horses, feline asthma bronchitis, broncho-pneumonia, tracheal hypoplasia, tracheal collapse AND as a uterus relaxant CONTRAINDICATIONS: Contraindicated in heart failure, arrhythmia and decreased mast cell degranulation - Not used in racehorses (because it is a doping agent) - Not used in food producing animals -> cause meat to have less fat content NOTE: Longer-Acting β2-Specific Drug

Answer 70

``` GROUP: Bronchodilator, β-adrenoceptor agonist and selective sympathomimetic (uterus relaxant) MOA: Agonism of the beta(2) receptor stimulates adenylyl cyclase activity which ultimately leads to downstream effects of smooth muscle relaxation in the bronchioles and uterus PK: Can be given SC and IV INDICATIONS: - Horse RAO - Feline asthma bronchitis - Broncho-pneumonia - Tracheal hypoplasia - Tracheal collapse - Uterus relaxant CONTRAINDICATION: Should be used cautiously in animals with diabetes, high blood pressure, overactive thyroid gland (hyperthyroidism) NOTES: Longer-Acting β2-Specific Drug. Less specific though! Given to dogs, cats and horses ```

Answer 71

GROUP: Phentothiazine (uterus relaxant) MOA: Sedation and uterus relaxatioace by inhibiting postsynaptic central dopaminergic receptors (alpha 1 receptor) PK: Large Vd, slow elimination, metabolise in liver, excretion in urine, bioavailability: PO-20% SE: Penile prolapse and hypertension in EQ, third eyelid prolapse in ca and fe, constipation, and dry mouth, paradoxical reactions INDICATION: Calming, sedation, muscle relaxation, premedication DOSE: Dog: PO: 1-2 mg/kg IM/IV: 0.2-0.3 mg/kg Horse: PO: 0.1-0.4 mg/kg IM/IV: 0.03-0.1 mg/kg

Answer 72

GROUP: Phentothiazine MOA: Block postsynaptic dopamine receptors → Uterus relaxation SE: Muscle necrosis when given IM. Cause excitation and tachycardia in eq. INDICATION: Psychotic disorders and uterus relaxation CONTRAINDICATION: Not recommended in horses due to extreme ataxia and altered mentation. Avoid use in patients that are dehydrated, hypovolemic, bleeding, or in shock because of the drugs effect on vessel tone (vasodilation).

Answer 73

GROUP: Tropane alkaloid (parasympatholytic) and uterus relaxant MOA: M-ACh antagonist. Interacts with muscarinic receptors of effector cells and, by occupying these sites, prevent ACh from binding to the receptor. PK: Well absorbed, crosses BBB, distributed in tissues, metabolize in liver and excretion via urine. Narrow TI (be careful with dosaging) SE: Excessive salivation and vomiting, increase in IOP, decrease tear production INDICATION: Cyclopegia, causes mydriasis, synechiae, iritis (inflammation of vascular membrane of the eye) and uterus stimulant CONTRAINDICATION: Patients with glaucoma or KCS (?) DOSE: Dog: IM, IV 0.02 mg/kg (OP poisoning 0.2-0.5 mg/kg IV 1/4, SC 3/4)

Answer 74

GROUP: Quaternary ammonium compound (parasympatholytic) and uterus relaxant MOA: Interacts with muscarinic receptors of effector cells and, by occupying these sites, prevent ACh from binding to the receptor. PK: Longer duration of action than atropine, safer to use, excretion in urine (I think) SE: Constipation, hypothermia, cough INDICATION: Pre-medication (decrease salivation) CONTRAINDICATION: Horses with colic

Answer 75

GROUP: Atropine derivative (M-ach antagonist and parasympatholytic) and uterus relaxant MOA: Non‐selectively blocking muscarinic receptors to cause mydriasis and cycloplegia PK: Rapid onset, short duration of action. SE: Confusion, tachycardia, unsteadiness INDICATION: Used in eye examinations and as uterine relaxant

Answer 76

GROUP: M- ACh antagonist (Parasympatholyitc) MOA: Interacts with muscarinic receptors of effector cells and, by occupying these sites, prevent ACh from binding to the receptor. PK: Short half-life. SE: Increase in heart-rate INDICATION: Antispasmodic - used in horses with colic and as a uterine relaxant CONTRAINDICATION: Horses with ileus

Answer 77

GROUP: Salicylates (classical NSAID's) MOA: It suppresses the production of prostaglandins and thromboxanes is due to its irreversible inactivation of the cyclooxygenase (COX) 1 and 2 enzyme (unsafe). PK: Used short-term. Generally good oral bioavailability in monogastric animals, penetrates BBB, metabolized in liver, excretion in urine SE: Irritating the stomach (vomiting), delayed healing, ren-and hepatotoxicity (it is considered an unsafe drug as it inhibit COX 1 and 2) INDICATION: Platelet aggregation inhibition (in thrombosis), analgesic and antipyretic CONTRAINDICATION: Do not use in cats, and after surgery

Answer 78

GROUP: ADP-receptor inhibitor (antiplatelet agent) MOA: is metabolized to its active form by carboxylesterase-1. The active form is a platelet inhibitor that irreversibly binds to P2Y12 ADP receptors on platelets -> Platelet aggregation PK: Medium absorption, high plasma binding, undergoes first pass metabolism, excreted 50/50 in urine and faeces. SE: Vomiting, diarrhoea (rare), inappetence. INDICATION: Inhibit thrombus formation (blood clotting)

Answer 79

GROUP: Anticoagulant (produced by mast cells) MOA: Inactivates clotting factors, binds to antithrombin, and this will lead to heparin amplifying the anticoagulant effect PK: Very ionised, no oral absorption, SC poor absorption, can be given IV, but SC preferred. SE: Heparin-induced thrombocytopenia (HIT syndrome) caused by an immunological reaction that makes platelets form clots within the blood vessels, stroke, myocardial infarction and disseminated intravascular coagulation INDICATION: Feline HCM, DIC, HeartWorm CONTRAINDICATION: Must monitor the activated partial thromboplastin time!

Answer 80

GROUP: Anticoagulant inhibitor (positive charge) MOA: Antagonist of heparin, binds to heparin so gets eliminated from the body PK: Given IV, slow infusion SE: Rare INDICATION: Decreased bleeding time

Answer 81

GROUP: Anticoagulant inhibitor (positive charge) MOA: It inhibits the effect of Prostacyclin which is the physiological antagonist of Thromboxanes in the body. Thromboxanes aggregate platelets and PGI prevents platelet aggregation. So if you inhibit the inhibitor, there will be platelet aggregation. PK: Given IV, , broad spectrum drug SE: Rare INDICATION: Decreased bleeding time, post surgery bleeding

Answer 82

GROUP: Alkylating agents MOA: It covalently binds to DNA --> Cyclophosphamide requires activation by the hepatic cytochrome P450. PK: Given PO or IV + mesna, should be given with a lot of water and the animal should be able to urinate throughout the day SE: Myelosuppression and neutropenia with thrombocytopenia to a lesser degree. GI toxicity can also be of concern but is more commonly encountered in cats. Cardiomyopathy, hemorrhagic cystitis, interstitial pneumonia, infection can also occur. INDICATION: Autoimmune diseases, leukemias (CLL*, orally) and lymphomas (and sarcomas?) NOTE: Intravenous administration of furosemide concurrently with cyclophosphamide has been shown to reduce the incidence of sterile hemorrhagic cystitis in dogs.

Answer 83

GROUP: Platinum compound (cytotoxic compound) STRUCTURE: They contain hydroxyl groups (aquation) MOA: Binding to DNA, RNA and proteins. Capable of producing a covalent cross-link between two nucleophilic atoms of a molecule. DNA cross-links are formed by binding sites on different DNA strands. These DNA lesions inhibit DNA replication and transcription and ultimately induce apoptosis (intrastrand crosslink) RESISTANCE: Resistance to the platinum agents can be through cytosolic inactivation of the drug secondary to glutathione conjugation or inactivation from other sulfhydryl-containing groups such as proteins. INDICATION: Osteosarcoma and carcinomas PK: Given IV, elimination is renal. SE: GI, myelosuppression, low nephrotoxicity

Answer 84

GROUP: Platinum compund (cytotoxic compund) STRUCTURE: They contain hydroxyl groups (aquation) MOA: Binding to DNA, RNA and proteins. Capable of producing a covalent cross-link between two nucleophilic atoms of a molecule. DNA cross-links are formed by binding sites on different DNA strands. These DNA lesions inhibit DNA replication and transcription and ultimately induce apoptosis (intrastrand crosslink) RESISTANCE: Resistance to the platinum agents can be through cytosolic inactivation of the drug secondary to glutathione conjugation or inactivation from other sulfhydryl-containing groups such as proteins. PK: Given IV or IP, elimination is renal. INDICATION: Osteosarcoma, carcinomas SE: GI+nephrotoxicity, myelosuppression, pulmonary edema (in cats) CONTRAINDICATION: Cats

Answer 85

GROUP: Anthracyclines MODA: Intercalates and binds to DNA, disrupting helical structure and DNA template, TII-mediated chain scission PK: Poorly bioavailable, given IV, elimination in bile and kidneys INDICATION: Lymphoma, leukemias, osteosarcoma, hemangiosarcoma SE: GI + myelosuppression, hemorrhagic colitis, arrhytmias, anaphylactoid reaction, congestive heart failure in dogs, cumulative nephrotoxicity in cats. Paravenous application: tissue irritation! PREVENTION: Dexrazoxan NOTE: Mitoxantrone is recommended "instead" as it has less side effects

Answer 86

GROUP: Vinca alkaloid MOA: Bind tubulin subunits and prevent microtubule polymerization PK: IV bolus, rapid decline in plasma concentration (drug distributes to peripheral tissues), slow elimination, metabolised in liver, and excreted in bile SE: Peripheral neuropathy (DL), myelosuppression, alopecia, gastrointestinal disturbance. Paravenous application: tissue irritation INDICATION: Lymphomas and sarcomas

Answer 87

GROUP: Tyrosine kinase inhibitors MOA: Inhibits tyrosine kinases, enzymes responsible for the activation of many proteins by signal transduction cascades. Specifically, masitinib targets the receptor tyrosine kinase c-Kit which is found to be overexpressed or mutated in several types of cancer. PK: Given PO with food, elimination in liver SE: Vomiting, diarrhea, azotemia, elevated liver enzymes, neutropenia INDICATION: Mast cell tumors in dogs NOTE: Monitoring: albumin, kidney function, WBC. The presence of a mutated form of the receptor protein c-kit in the tumours should be confirmed before the start of treatment.

Answer 88

GROUP: Iodophores (halogenated) MOA: Iodine is solubilized by surfactants, remain in a dissociable form. Slow contimual release of free iodine PK: pH<4, ANTIMICROBIAL SPECTRUM: Bacterias, viruses and fungi INDICATION: Teat dips, dairy sanitizers, General antiseptic for various dermal and mucosal infections, surgery

Answer 89

GROUP: Inorganic chlorines (halogens) MOA: Germicidal → denature proteins PK: Unstable in sunlight, inactivated in presence of blood, strong odour SE: Irritation of mucous membranes INDICATION: Bleach, coagulation (water, sewage treatment) NOTE: Corrosive to metals

Answer 90

GROUP: Biguanides STRUCTURE: Synthetic cationic compound MOA: Cell membrane disruption ANTIMICROBIAL SPECTRUM: Gram+ > Gram- bacteria, Mycobacterium tuberculosis, fungi, poor against viruses, not against spores. Dermatology – bacteria, yeasts (Malassezia spp, Candida spp), but less effective against dermatophytes PK: pH dependent, rapid action, longest residual activity SE: Extremely low toxicity INDICATION: One of the most commonly used surgical and dental antiseptics: Skin treatment, ear treatment, wound treatment (e.g. 1% chlorhexidine-acetate), shampoos, soaps, teat dips NOTE: Combination with alcohol and in combination with drugs

Answer 91

GROUP: Alkyalting agents MOA: Its biocidal activity is related to its ability to alkylate sulfhydryl, hydroxyl, carboxyl, and amino groups affecting RNA, DNA, and protein synthesis PK: Oil, good germicidal activity, penetrates blood, coagulating proteins. It retains its biocidal activity in the presence of organic matter, noncorrosive to metal SE: Irritative to eyes and nasal passages ANTIMICROBIAL SPECTRUM: It has better bactericidal, virucidal, and sporicidal activity than formaldehyde INDICATION: Sterilize instruments CONTRAINDICATION: Must be used in well-ventilated areas

Answer 92

GROUP: Alcohol STRUCTURE: Primary alcohol, a hydrogen is substituted with a hydroxy group MOA: Proteine penetration (?) PK: Germicidal, lipid soluble, can penetrate proteins ANTIMICROBIAL SPECTRUM: Most vegetative gram-positive, gram-negative, and tubercle bacillus organisms. INDICATION: Skin disinfectants, capillary dilation. CONTRAINDICATION: High level disinfection (inactivity against bacterial spores and reduced efficacy in the presence of protein or other bioburden) NOTE: After repeated and prolonged use, alcohols can damage the shellac mounting of lensed instruments, can swell or harden rubber and certain plastic tubing

Answer 93

GROUP: Peroxides MOA: Release of nascence oxygen, protein damage. Wound surface/mucus membrane - catalase liberates O2 PK: Short duration, limited to superficial layer of surface, limited use in wound treatment ANTIMICROBIAL SPECTRUM: Bacteria, yeasts, fungi, viruses – no/little effect on spores INDICATION: Disinfection dental and surgical instruments, water treatment, food industry

Answer 94

GROUP: Peroxides MOA: Release of nascence oxygen, protein damage. ANTIMICROBIAL SPECTRUM: Bacteria, yeasts, fungi, viruses (0.001%–0.003%) spores (0.25%–0.5%) PK: Short effect INDICATION: Food industry (meat and poultry processing plants and dairies) IN COMBINATION: peracetic acid (0.23%) and hydrogen peroxide (7.35%)

Answer 95

GROUP: Quaternary Ammonium Compound MOA: Change cell membrane permeability, disruption ANTIMICROBIAL SPECTRUM: Bacteria, some fungi, protozoa. Not against viruses and spores ACTIVITY REDUCTION: By porous or fibrous materials, anionic substances (e.g., soaps, proteins, fatty acids, phosphates), presence of blood and tissue debris INDICATION: Cleaning surfaces, antiseptics, teat dips

Answer 96

GROUP: Azo dyes MOA: Activates in an acidic medium ANTIMICROBIAL SPECTRUM: Gram - negative bacteria. INDICATION: Scarlet red 5% ointment: sores, ulcers, wounds. Pyridium: often incorporated as an analgesic with sulfonamides to treat urinary tract infections (NOTE: THIS IS NOT INCLUDED IN TOPIC 25 OR 26 BUT WE WERE ASKED TO LEARN ONE DYE!)

Answer 97

GROUP: Organomercury compounds (metal) MOA: Enzyme inhibition- SH groups PK: Decreased use - environmental persistence and contaminant potential, toxicity (NOTE: THIS IS NOT INCLUDED IN TOPIC 25 OR 26 BUT WE WERE ASKED TO LEARN ONE METAL!)

Answer 98

GROUP: Antiprotozoal against leishmaniasis MOA: Inhibits protein synthesis on 16S ribosomal subunit PK: PO: Poor absorption, but PO is less toxic than injection, elimination via kidneys mainly in unchanged form SE: Irreversible cochlear, and renal toxicity i.e. kidney and ear (like aminoglycosides), nausea, diarrhea ANTIMICROBIAL SPECTRUM: Cryptosporidiosis and amoeba infection, histomoniasis, visceral leishmaniasis INDICATION: Against leishmania. Use as feed additive for the control of Histomonas meleagridis in turkeys. CONTRAINDICATION: Previous renal disease, individuals with a history of previous hypersensitivity reactions. Also contraindicated in intestinal obstruction

Answer 99

GROUP: Agent against leishmaniasis MOA: It effects apoptosis and disturbance of lipid-dependent cell signalling pathways --> Cell death PK: PO administration, good distribution, penetrates the BBB SE: : Relatively non-toxic, vomiting, foetotoxic, teratogenic ANTIMICROBIAL SPECTRUM: Broad spectrum phospholipid local anticancer and antimicrobial drug, bacterial, fungal, and amoeba infection + Leishmaniasis IN COMBINATION: Marbofloxacin and/or allopurinol

Answer 100

GROUP: Nitroimidazoles STRUCTURE: Nitroimidazole derivative MOA: In anaerobic conditions toxic metabolites (nonenzymatic reduction of the nitro group) destroy the DNA of bacteria or protozoa ANTIMICROBIAL SPECTRUM: Obligate anaerobic bacteria: Clostridium spp.Bacteroides spp. Fusobacterium spp. Brachyspira hyodysenteriae. Protozoa: Trichomonas spp. Histomonas spp. Giardia spp. Amoeba spp. PK: Excellent absorption, tissue penetration, CSF, prostate, metabolisation in liver, elimination via kidney SE: Stomach pain, breathing difficulty, pounding heartbeat INDICATION: Gingivitis, paradontitis, periodontitis, oral cavity infections, Anal sacculitis, Pseudomembranous colitis! (Cl. difficile, Cl. perfringens), Trichomonas, Giardiosis! Histomonosis CONTRAINDICATIONS: Banned for Swine dysentery prevention, D (Prudence) category

Answer 101

GROUP: Nitroimidazole (carbamate ester) MOA: In anaerobic conditions toxic metabolites (nonenzymatic reduction of the nitro group) destroy the DNA of bacteria or protozoa ANTIMICROBIAL SPECTRUM: Obligate anaerobic bacteria: Clostridium spp.Bacteroides spp. Fusobacterium spp. Brachyspira hyodysenteriae. Protozoa: Trichomonas spp. Histomonas spp. Giardia spp. Amoeba spp. PK: Excellent absorption, tissue penetration, CSF, prostate, metabolisation in liver, elimination via kidney SE: Stomach pain, breathing difficulty, pounding heartbeat INDICATION: Gingivitis, paradontitis, periodontitis, oral cavity infections, Anal sacculitis, Pseudomembranous colitis! (Cl. difficile, Cl. perfringens), Trichomonas, Giardiosis! Histomonosis CONTRAINDICATIONS: Banned for Swine dysentery prevention, D (Prudence) category

Answer 102

GROUP: Proenzimidazole (prodrug) and banzimidazole carbamate STRUCTURE: Benzimidazole carbamate MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNINTIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. It also has larvicidal and ovicidal effect. Anticestodal effect (AC): Against tapeworms PK: Limited absorption from GI. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: Given PO as a suspension, paste, bolus or premix in slow release capsule (140 days in sheep and goat), other uses: Antitumor, antifungal, antiviral, antiparasitic. NOTES: High levels and repeated administration may be necessary in horse. WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 103

GROUP: Benzimidazole (carbamate) STRUCTURE: Synthetic benzimidazole derivative MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNINTIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. It also has larvicidal and ovicidal effect. Anticestodal effect (AC): Against tapeworms Antitrematodal effect (AT): Dicrocoelium, Paramphistomum spp.) (only for adult stages) PK: Absorption from GI, reversibly oxidized to its sulphoxide (which gives poor binding to parasite β-tubulin. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: Given PO as a suspension, paste, bolus or premix in slow release capsule (105 days in ruminants), other uses: Antitumor, antifungal, antiviral, antiparasitic. NOTES: Has been shown to inhibit the enzyme fumarate reductase, which is helminth specific. WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 104

GROUP: Probenzimidazole (prodrug) STRUCTURE: Halogenated benzimidazole carbamate MOA: Inhibition of tubulin polymerization -- > binding to colchicine sensitive site of tubulin RESISTANCE: Recently more frequent. Ruminants, GI roundworms, frequently as multiple resistance against BZs. In horse: Large strongyles, and in swine: Oesophago-stomum spp ANTIHELMNINTIC SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. It also has larvicidal and ovicidal effect. Anticestodal effect (AC): Against tapeworms PK: Limited absorption from GI. Excretion in bile and elimination via faeces SE: PO relatively safe, teratogenicity, hepatotoxicity, neurotoxicity INDICATION: Given PO as a suspension, paste, bolus or premix to horse, cats, dogs and ruminants, other uses: Antitumor, antifungal, antiviral, antiparasitic. CONTRAINDICATION: Might be necessary with off-label use in horse and WP is 8-14 days for meat, except boluses which are more than 3 months.

Answer 105

GROUP: Carbanilide derivatives STRUCTURE: Aromatic urea derivative MOA: They bind to DNA and interfere with replication. Babesicidal and trypanocidal effects ANTIMICROBIAL SPECTRUM: Babesiosis PK: Strong binding to tissues, long WP (meat 90, milk 21 days) SE: Transient vomiting, pain and swelling on injection site INDICATION: Treatment and prophylaxis (prevention) of babesiosis, + anaplasmosis and ehrlichiosis CONTRAINDICATION: High efficacy, but toxic drug, small TI

Answer 106

GROUP: Tetracyclines (short-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: Ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica (BABESIA) Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia PK: Lipophilic with excellent pharmacokinetics, penetrating inside all cells and crossing all biological membranes and barriers SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo CONTRAINDICATIONS: Never combine with aminoglycosides NOTES: Normal for human use

Answer 107

GROUP: Tetracyclines (short-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: Ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica (BABESIA) Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia PK: Lipophilic with excellent pharmacokinetics, penetrating inside all cells and crossing all biological membranes and barriers SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo CONTRAINDICATIONS: Never combine with aminoglycosides NOTES: Normal for human use

Answer 108

GROUP: Tetracyclines (short-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica (BABESIA) Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia PK: Lipophilic with excellent pharmacokinetics, penetrating inside all cells and crossing all biological membranes and barriers SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo

Answer 109

GROUP: Tetracyclines (long-acting) STRUCTURE: Linear fused tetracyclic nucleus MOA: Passively diffuse through porin channels in the bacterial membrane and inhibit 30S ribosomal subunit and thus inhibit bacterial protein synthesis MODA: Bacteriostatic ; at high concentration it is bactericidal RESISTANCE: ab ovo: Pseudomonas aeruginosa. Acquired: E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica, Staphylococcus aureus, Streptococci ANTIMICROBIAL SPECTRUM: Intracellular bacteria: Chlamydophilae, Rickettsia, Ehrlichia, Lawsonia, etc. Mycoplasma haemofelis, Bordetella bronchiseptica, Wolbachia, Plasmodium & Entamoeba histolytica (BABESIA) Almost all Gram positive Bacteria: Bacillus, Clostridium, Staphylococcus, Streptococcus etc.. Fastidious Gram negative bacteria: Pasteurella, Haemophilus, Actinobacillus etc... Enterobacteriaceae: E. coli, Salmonella, Klebsiella Anaerobics: Bacteroides, Fusobacterium, Proteus Spirochaetes: Leptospira, Borrelia. Toxoplasmosis! PK: More lipophilic with excellent absorption, penetrate bone, low degree of metabolism and mainly excreted via the large intestine in the bile SE: Tissue irritant, vomiting, diarrhea, hepatoxicity, impairment of bone growth in very young animals INDICATION: General infections, most respiratory infections, bronchopneumonia, foot diseases, metritis, mastitis, Mycoplasma respiratory infections in Ru/Su/Av, Infectious keratoconjunctivitis in Bo NOTES: First choice against Lyme disease, lethal proliferative enteropathy in horse

Answer 110

GROUP/STRUCTURE: Synthetic isoquinoline pyrazine derivative MOA: Induction of spastic paralysis in the parasite. RESISTANCE: No resistance reported in adult parasites ANTIMICROBIAL SPECTRUM: Highly effective against cestodes of ruminants. All species of Moniezia, Stilesia, and Avitellina of sheep and/or goats are eliminated by a single dose PK: Rapid and almost complete absorption of the GI! Distribution: To all organs. Secretion: Bile SE: Wide safety margin, practically non-toxic (TI=50) INDICATION: Ruminants: PO (Moniezia spp., Stilesia), Horses: PO (Anoplocephala perfoliate) Poultry: PO, Cats and dogs: PO or SC

Answer 111

GROUP: Benzene sulfonamide STRUCTURE: Aminobenzene disulphon amide derivative RESISTANCE: Active against nematodes that are resistant to other anthelmintics. ANTIMICROBIAL SPECTRUM: Relatively narrow, GI nematodes (including hypobiotic larvae) PK: In plasma is bounded to proteins. Renal excretion of the parent drug is thought to be the main route of elimination. Safety margin is wide INDICATION: Sheep PO suspension for infections with (mainly) adult liver flukes. Cattle SC injection in combination with Ivermectin. CONTRAINDICATION: Not licensed for use in lactating dairy cows

Answer 112

GROUP: Aminoacetonitrile derivatives MOA: Agonist on nicotinic receptors of worms RESISTANCE: Active against nematodes that are resistant to other anthelmintics. ANTIMICROBIAL SPECTRUM: Relatively narrow, GI nematodes (including hypobiotic larvae) PK: Absorption from GI is good. Rapid metabolization to sulfoxide and sulfone metabolites. Excretion with faeces, via bile INDICATION: Against nematodes

Answer 113

GROUP: Semisynthetic antibiotics STRUCTURE: Cyclooctadepsi-peptide MOA: Inhibition on synaptic transmission, by binding to a group of G-protein coupled receptors called latrophilins, inhibiting muscle in nematodes RESISTANCE: Is a resistance breaking anthelmintic ANTIMICROBIAL SPECTRUM: Antinematodal effect (AN): Broad spectrum of activity against roundworms. SE: Safe drug, rare ADRs (licking, excessive grooming, salvitaion, lethargy, etc..) INDICATION: Is effective against a number of GI nematodes, roundwoms, hookworms. Licensed for use in combination with Praziquantel in cats for topical application, in dogs for oral application NOTE: Excellent activity against Toxacara cati (mature and immature adults)

Answer 114

GROUP: Purine analogue MOA: Competitively inhibit DNA polymerase of the virus. In the course of phosphorylation, the viral thymidin-kinase binds it 20 times more efficiantly than the host. Irreversible binding to DNA-polymerase → very effective VIRAL SPECTRUM: Only DNA-viruses INDICATION: Herpes in cats and labial, genital herpes and Epstein-Barr in humans PK: PO, IV and locally as eye drop, eye ointment and cream

Answer 115

GROUP: Purine analogue MOA: Competitively inhibit DNA polymerase of the virus. In the course of phosphorylation, the viral thymidin-kinase binds it 20 times more efficiantly than the host. INDICATION: Against humans cytomegalovirus. PK: Only IV → mainly humans

Answer 116

GROUP: Purine analogue MOA: Competitively inhibit DNA polymerase of the virus. In the course of phosphorylation, the viral thymidin-kinase binds it 20 times more efficiantly than the host. INDICATION: Only used in cats. Should be converted to penicoclover but this conversion is lower in cats. Keratitis, Rhinitis, FHV, Dermatitis

Answer 117

GROUP: Interferon MOA: Prevents penetration, replication and assembly of viruses (antigen-presentation↑, NK, T-killer activity ↑) INDICATIONS: FeLV (combination with Zidovudine → interferon omega), Parvovirus, FIP, Herpes NOTE: Main inductor: DS RNA INF alpha, beta, gamma, omega Have questionable results, are expensive

Answer 118

GROUP: Interferon MOA: Prevents penetration, replication and assembly of viruses (antigen-presentation↑, NK, T-killer activity ↑) INDICATIONS: FeLV (combination with Zidovudine → interferon omega), Parvovirus, FIP, Herpes NOTE: Main inductor: DS RNA INF alpha, beta, gamma, omega Have questionable results, are expensive

Answer 119

GROUP: Alkylating agents MOA: It covalently binds to DNA --> Cyclophosphamide requires activation by the hepatic cytochrome P450. PK: Given PO or IV + mesna, should be given with a lot of water and the animal should be able to urinate throughout the day SE: Myelosuppression and neutropenia with thrombocytopenia to a lesser degree. GI toxicity can also be of concern but is more commonly encountered in cats. Cardiomyopathy, hemorrhagic cystitis, interstitial pneumonia, infection can also occur. INDICATION: Autoimmune diseases, leukemias (CLL*, orally) and lymphomas (and sarcomas?) NOTE: Intravenous administration of furosemide concurrently with cyclophosphamide has been shown to reduce the incidence of sterile hemorrhagic cystitis in dogs.

Answer 120

GROUP: Platinum compound (cytotoxic compound) STRUCTURE: They contain hydroxyl groups (aquation) MOA: Binding to DNA, RNA and proteins. Capable of producing a covalent cross-link between two nucleophilic atoms of a molecule. DNA cross-links are formed by binding sites on different DNA strands. These DNA lesions inhibit DNA replication and transcription and ultimately induce apoptosis (intrastrand crosslink) RESISTANCE: Resistance to the platinum agents can be through cytosolic inactivation of the drug secondary to glutathione conjugation or inactivation from other sulfhydryl-containing groups such as proteins. INDICATION: Osetosarcoma and carcinomas PK: Given IV, elimination is renal. SE: GI, myelosuppression, low nephrotoxicity

Answer 121

GROUP: Platinum compund (cytotoxic compund) STRUCTURE: They contain hydroxyl groups (aquation) MOA: Binding to DNA, RNA and proteins. Capable of producing a covalent cross-link between two nucleophilic atoms of a molecule. DNA cross-links are formed by binding sites on different DNA strands. These DNA lesions inhibit DNA replication and transcription and ultimately induce apoptosis (intrastrand crosslink) RESISTANCE: Resistance to the platinum agents can be through cytosolic inactivation of the drug secondary to glutathione conjugation or inactivation from other sulfhydryl-containing groups such as proteins. PK: Given IV or IP, elimination is renal. INDICATION: Osteosarcoma, carcinomas SE: GI+nephrotoxicity, myelosuppression, pulmonary edema (in cats) CONTRAINDICATION: Cats

Answer 122

GROUP: Anthracyclines MODA: Intercalates and binds to DNA, disrupting helical structure and DNA template, TII-mediated chain scission PK: Poorly bioavailable, given IV, elimination in bile and kidneys INDICATION: Lymphoma, leukemias, osteosarcoma, hemangiosarcoma SE: GI + myelosuppression, hemorrhagic colitis, arrhytmias, anaphylactoid reaction, congestive heart failure in dogs, cumulative nephrotoxicity in cats. Paravenous application: tissue irritation! PREVENTION: Dexrazoxan NOTE: Mitoxantrone is recommended "instead" as it has less side effects

Answer 123

GROUP: Vinca alkaloid MOA: Bind tubulin subunits and prevent microtubule polymerization PK: IV bolus, rapid decline in plasma concentration (drug distributes to peripheral tissues), slow elimination, metabolised in liver, and excreted in bile SE: Peripheral neuropathy (DL), myelosuppression, alopecia, gastrointestinal disturbance. Paravenous application: tissue irritation INDICATION: Lymphomas and sarcomas

Answer 124

GROUP: Tyrosine kinase inhibitors MOA: Inhibits tyrosine kinases, enzymes responsible for the activation of many proteins by signal transduction cascades. Specifically, masitinib targets the receptor tyrosine kinase c-Kit which is found to be overexpressed or mutated in several types of cancer. PK: Given PO with food, elimination in liver SE: Vomiting, diarrhea, azotemia, elevated liver enzymes, neutropenia INDICATION: Mast cell tumors in dogs NOTE: Monitoring: albumin, kidney function, WBC. The presence of a mutated form of the receptor protein c-kit in the tumours should be confirmed before the start of treatment.

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