midterm 1 - drugs

Phenobarbital:

MOA, adverse effects and monitoring?

MOA: binds to GABA receptor, inhibitory effect, releases acetylcholine, norepinephrine, glutamate. Tolerance via induction of cytochrome p450

Adverse effect: anxiety, sedation, ataxia, polyuria, Increase ALP/ALT, hepatotoxicity and liver failure

Monitoring: routine CBC/Chem

• C-IV

Potassium Biomide:

MOA, adverse affects, monitoring

MOA: GABA receptor, affect chloride ions and membrane hyperpolarization

Effects: sedation, ataxia, hyperactivity, vomiting, polyuria, pancreatitis

Monitoring: CBC,Chem, urinalysis

• metabolized in kidneys

• narrow therapeutic range

• avoid in cats→ pulmonary symptoms

Diazepam:

MOA, adverse effects, monitoring

MOA: binds to GABA receptor and increase affinity for GABA

Effects: sedation, excitatory, caution w/ cats → liver failure and aggressive animals, appetite

• IV during seizure

• PO only for short duration

• C-IV

Midazolam:

MOA, adverse effects, monitoring, given how?

MOA: binds GABA receptor and increase affinity for GABA

Effects: respiratory depression

• C-IV

• in anesthesia protocol

• 3x potent than diazepam

• IV, IM, Intranasal

Lorazepam (Ativan):

MOA, adverse affects, monitoring

MOA: binds GABA receptor and increase affinity for GABA

Effect: increased appetite, ataxia, vocalization, caution w aggression

• C-IV

• not metabolized by liver

Propofol:

MOA: potentiates GABA stronger to produce faster effects, anesthetic induction agent → short-acting

Effect: apnea and arrhythmias

• used for status epilepticus thru IV

Levetiracetam (Keppra):

prevent spread of seizure activity, not metabolized by liver

effects: sedation, ataxia, reduced appetite

• wide therapeutic range w/ limited adverse effects

Zonisamide:

MOA: unknown but can possible affect Na and Ca channels

Effects: ataxia and sedation

• given Oral BID

Gabpentin:

MOA: inhibit Ca channels to decrease excitatory neurotransmitter

Effect: analgesia, anxiolytic (cats)

• related to GABA but not affect GABA, it stops Ca

• Gaba→ directely provides inhibitory

Clorazepate:

• C-IV benzodiasepine

• with phenobarb

Clonazepam:

how is the usage different from dog and cat

• C-IV benzodiazepine

• dogs → short term use

• cats → long-term use

Acepromazine:

• blocks CNS dopamine receptors for primary effect

• Can lead to hypotension since alpha 1 is blocked → vasodilation → ↓ BP → hypotension

• has alpha 1 adrenergic receptor antagonist

Effect: hypotension, 3rd eyelid protrusion, reduce aggression inhibition, reduce platelet aggregation

• dogs, cats, horses

• IV, IM, subQ or oral

• liver metabolism

All benzodiazepines can also be?

Anxiolytic and muscle relaxation

• binds GABA receptor and increase affinity for GABA

• no analgesia

• Not FDA approved

Effects: agitation, weakness, feline liver failure w/ oral

Alpha-2 Adrenergic agonists:

MOA, Adverse effects

MOA: bind and stimulate alpha-2 adrenergic receptor

Effects: CNS depression, bradycardia, hypertension, analgesic

• kitty/doggy magic

• reversible

Alpha-2 adrenergic agonists

Dexmedetomidine

• dogs and cats

• IV, IM, SubQ

• effect within 15 min

Alpha-2 Adrenergic Agonist:

Xylazine

• horses and cattle

• IV, IM, SubQ

• combo with ketamine

Reversal Agent for alpha-2 antagonist:

Atipamezole

reversal of dexmedetomidine

Effects: vomiting, diarrhea, hypersalivaiton

Reversal Agent for alpha-2 antagonist:

Yohimbine

reversal for Xylazine

Effects: muscle tremors and salivation

What are opioids? what are its side effects

analgesia, sedation, and relieve anxiety

Effects: mild sedation, respiratory depression, bradycardia, hypothermia

Opioid → Mu agonist:

Morphine

may cause histamine release

Effect: vomiting and defecation and dysphoria in cats and horses

Opioid → Mu agonist:

Fentanyl

synthetic opioid, 100x MORE potent than morphine

• PPE

Opioid → Mu agonist:

Hydromorphone

synthetic, 5-7x potent than morphine

Effect: vomiting, resp depression, cats hyperthermia

Opioid → Mu agonist:

Oxymorphone

synthetic, 10x potent than morphine

• only for dogs

Opioid → Mu agonist:

Methadone

synthetic opioid but also a NMDA receptor

MOA: prevents excitability of pain pathways

Effects: similiar to other opioids but less sedating and less vomiting

Opioid → Mu agonist:

Hydrocodone

synthetic but can be oral cough suppressant

Partial Mu agonist:

Buprenorphine (simbadol)

• 30x potent than morphine

• delayed onset-45/60 min

• transmucosal has first-pass effect

• primary opioids for cats

Mixed Kappa Agonist and Mu Antagonist:

Butorphanol

• antitussive

• sedative based on kappa receptor

• less resp depression

• will reduce analgesia of pure mu agonist if given together

Opioid Antagonist:

Naloxone

• high opioid receptors

• reverses analgesic effect

Local anesthetics:

Lidocaine

rapid around 5-15 min with short duration of 1-2 hr

• accidental IV can give cardiac arrest

Local anesthetics:

bupivacaine

rapid onset but longer duration 4-6 hr b/c of higher molecular weight

• accidental IV can lead to cardiovascular

Local anesthetics:

Proparacaine

In the cornea

Dissociative Agents:

Ketamine → affects? Used?

Effects: catalepsy (loss of consciousness w/ muscle rigitity) amnesia, analgesia

• MOA-NMDA receptor antagonist = controls synaptic memory and learning

• used for induction and sedation

• Kitty magic

dissociative agents:

tiletamine/Telazol

• short sedation

• pain on injeciton

• pre-euthansia

General anesthetic:

Propofol

• short acting injectable

• cats should only be given this one time only

• MOA increases binding of GABA to GABA-R

General anesthetic:

Alfaxalone

• IV or IM

• no analgesia

• neuroactive steroid binding GABA receptor

• fast metabolized in liver → short acting but longer w pt’s hepatic disease

General anesthetic:

Etomidate

• no analgesia

• binds GABA receptor

• metabolized by liver

• minimal cardiovascular and mild respiratory dep

CNS drugs name 2:

Doxapram and Pentobarbital

Doxapram: stimulates brainstem to increase respiration

Pentobarbital: CNS depression via inhibition and effect GABA receptor

Anticholingergic:

Atropine

prevent or treat bradycardia

• IV within 1 min

Anticholingergics:

Glycopyrrolate

prevent and treat bradycardia

• slower onset but longer duration

SNS adrenergic:

Epineprhine, adverse effect

Effect: tachycardia, hypertension and cardiac arrhythmias

MOA: increase HR and CO, vasoconstrictm brochodilation

• non-selective alpha 1, beta 1 and 2

SNS adrenergic:

Dobutamine, effects

Effect: tachycardia, hypertension and cardiac arrhythmias

MOA: treat hypotension during anesthesia

• monitor for arrhythemias

• selective for beta 1, mild on beta2and alpha 2 activity

SNS adrenergic:

dopamine

• selective on bata 1 and alpha 1

• monitor for arrhythmias

• positive inotrope →incr CO → incr BP

Effect: tachycardia, hypertension and cardiac arrhythmias

SNS adrenergic:

Norepinephrine

• non-selective

• CRI for hypotension

SNS adrenergic:

Isoproterenal

• selective on beta 1 and 2

• brochodilation, incr HR

SNS adrenergic:

Phenylpropanolamine

used to treat urinary incontinence

SNS adrenergic:

Albuterol

selective on beta 2

• treat brochospasm

SNS adrenergic:

Ephedrine

stimulates release of endogenous to treat hyptension

SNS adrenergic antagonists:

Phenoxybenzamine

decrease urinary sphincter tone for blocked male cats

laminitis in horses

SNS adrenergic antagonists:

Prazosin

relax urinary sphincters in blocked male cats

SNS adrenergic antagonists:

propranolo

treat cardiac arrhythmias

SNS adrenergic antagonists:

Metoprolol and Atenolol

treat hypertension

SNS adrenergic antagonists:

Timolol

block bet 1 AND 2

for glaucoma treament

Cardiac → Positive Inotropes:

Digoxin and Digitoxin

MOA: increase contraction force by inhibiting Na/K pump → increase intracellular Ca

Effects: CHF, tachycardia

Monitor: blood levels b/c of low margin of safety

• from foxglove plant

Catecholamines:

Epinephrine

Causes: vasoconstriction, incr HR and contractility, brochodilation

• used for emergencies → anaphylaxis and cardiac arrest

Effects: arrhyrthmias and hypertension

Catacholamines:

Dopamine

is a norepinephrine precursor → a1 and beta 1

• increase HR and contractility

Effect: Tachycardia and arrhythmia

Uses: cardiac arrest, severe shock

Catecholamines:

Dobutamine

its beta 1

• increases contractiliy without tachycardia

Vasoconstrictors:

Vasopressin

increase peripheral vasoconstriction and fluid retention

• increase BP

• it is anti-diuretic hormone ADH

ACE inhibitors:

Enalapril

renal elimination

• Prevent conversion of Angiotensin I to Angiotensin II

Monitor: kidney levels and ACE reduces GFR

Effects: GI and hypotension

ACE inhibitor:

Benazepril

renal and hepatic elimination

• Prevent conversion of Angiotensin I to Angiotensin II

Monitor: kidney levels and ACE reduces GFR

Effects: GI and hypotension

Angiotensin 2 Receptor Blocker:

Telmisartan

reduces vasoconstriction and lower BP

• for feline hypertension

Effects: weight loss, lethargy

Inodilator:

Pimobendan (vetmedin)

approved for management of CHF it is first in line treatment

MOA: incr contractility and vasodilation → incr SV

Effects: Anorexia, lethargy, diarrhea, dyspnea

• phosphodiesterase 3 inhibitors PDE3 = involved w cardiac relaxtion

Diuretics:

Furosemide

incr urine volume produce by kidneys by inhibiting the reabsorption of sodium and chloride

• reduces BP and pulmonary edema

Phosphodiesterase 5 inhibitor

Slidenafil

used to treat pulmonary hypertension as it can cause stress on R heart

• selective vasodilation

Calcium Channel Blocker

Amlodipine

vasodilator to treat hypertension

• more effective than ACE inhibitor for cats

Monitor: BP for hypotension

Calcium Channel Blocker

Diltiazem

treats atrial fibrillation and relax the myocardium

affect AV node cell → slows conduction → decr tachycardia

Anticoagulants:

Heparin

inhibit clot formation

• prevent conversion of prothrombin to thrombin

Anticoagulants:

EDTA

bind to Ca to prevent clot formation

• inhibit clot formation

Anticoagulants:

Coumarin derivatives

bind to Vitamin K to inhibit synthesis of clotting factors

Anticoagulants:

Aspirin

inhibit platelet aggregation

Pro-coagulant drugs (hemostatic):

Vitamin K

needed for formation of clotting factors

• treatment for rodenticide toxicity

Pro-coagulant drugs (hemostatic)

Protamine sulfate

binds heparin as there might be heparin overdose

Pro-coagulant drugs (hemostatic)

Silver Nitrate sticks

stop capillary bleeding

Respiratory drugs:

Expectorants

increase mucus reducing stickiness of mucus

• believed to increase flow of respiratory secretions to clear airway

Respiratory drug

Mucolytics

decrease viscosity or thickness of respiratory secretions

Res drugs

Antitussives → Dextromethorphan and Temaril P

suppress coughing

• dextromethorphan : OTC and central acting

• Temaril P : central acting cough suppressant and treat inflammatory coughs

Res drugs

decongestants

decrease swelling of nasal passages

• given spray, orally

used to treat feline upper respiratory tract dz

Res drug

Bronchodilators → Epinephrine, Isoproteronol, Terbutaline, Albuterol

are produced by stimulating activity of SNS or by suppressing activity of PNS

• Epinephrine and isoproteronol have short term emergency use and has heart stimulating effects

• Terbutaline and albuterol more selective for B1/2, less cardiac stimulation

• Aminophylline and Theophylline: inhibit phosphodiesterase → promotes brochoconstriction. Amino is metabolized into theophylline

Res drug:

Antihistamines

histamine block

• reduce other allergy symptoms such as discharge and sneezing

Effect: CNS depression, dry mouth, urinary retention

• drugs ending in -amine

Res drug

Respiratory stimulants → doxapram

stimulates animal to increase ventilation activity

• Doxapram: CNS stimulant used in neonates after C-section or dystocia

• used to restore reflexes after anesthesia

Effects: hypertension, arrhythmias