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97 Cards in this Set

  • Front
  • Back
What are the classifications of drugs acting in the ANS?
drugs acting on the parasympathetic
drugs acting on sympathetic
all by stimulation or inhibition
What are the two catagories under parasympathomimetics?
direct-acting
indirect acting (only by one mechanism by inhibiting choline esterases)
What are drug examples of parasympathomimetics?
Choline esters like Carbachol and Bethanechol

Cholinominetic alkaloids
Muscarine and pilocarpine
What are the effects of Ach?
vasoconstriction of bronchi
vasodilation
decrease cardiac output (M2)
increased GI motility
constriction of pupil
increase micturition
contractility of skeletal muscle
What is carbachol?
Direct acting
Classification: synthetic ester
Mechanism: Muscarinic and nicotinic agonist
Clinical uses: open angle glaucoma
Problems: systemic vasodilation
Pharmacokinetics - give IV, not very lipid soluble
What is Bethanechol?
Direct acting
Classification: Synthetic parasympathomometic
Mechanism: Muscarinic agonist
Clinical uses: Postoperative nonobstructive urinary retention
Problems: severe systemic cardiac affects
Pharmacokinetics: give orally or SC not IM or IV

Acetylcholinesterase does not inactivate bethanechol
A quaternary ammonium compound
Ionize non lipid soluble
What is Pilocarpine?
Direct acting
Classification:Tertiary alkaloid
Mechanism: muscarinic agonist
Clinical uses: Open-angle glaucoma and to increase tear secretion. Which counter acts the mydriatic effect of sympathomimetic drugs
Problems: systemic effects
Pharmacokinetics: use locally

Used with atropine to break the adhesion between the iris and the lens
What drugs are indirect acting reversible parasympathomimetics?
Physostigmine
Neostigmine
Edrophonium
Pyridostigmine
Demecarium
What is Physostigmine?
indirect acting reversible parasympathomimetic
Classification: a tertiary amine
Mechanism: counter acts central and peripheral effects of anticholinergic drugs like atropine
Clinical uses: used as an opthamnic agent for open angle glaucoma
Problems: use caustion with patients with seizure disorders
Pharmacokinetics: administered parenterally IV or IM and topically on the eye
crosses the BBB
What is Neostigmine?
Classification: A quaternary amine
Mechanism: to antagonize the effects of nondepolarizing muscle
Clinical uses: used to treat and diagnose myasthenia gravis, can stimulate GI motility and treat postoperative nononstructive urinary retention
Problems:
Pharmacokinetics: given orally and parenterally (IV or IM)

Has a longer duration than edrophonium
What is Edrophonium?
Classification: a quaternary amine
Mechanism: Indirect acting parasympathomimetic
Clinical uses: used for diagnosing myasthenia gravis
Problems: less adverse side effects because of short duration of action
Pharmacokinetics: admimistered IM or IV
What is Pyridomstigmine?
Classification: a quaternary amine
Mechanism: Indirect acting parasympathomimetic
Clinical uses: used for treating myasthenia gravis
Problems:
Pharmacokinetics: admimistered IM or IV

Atropine is used to treat toxicity of cholinesterase
What is Demecarium?
Classification: a carbamate reversible cholinesterase inhibitor
Mechanism: Indirect acting parasympathomimetic
Clinical uses: used for open angle glaucoma, topical ophthalmic miotic agent
Problems: long duration of action organophosphates (12-48hrs)
Pharmacokinetics: used topically
What are drugs that are opthamic organophosphates?
Echthiophate
Isoflurophate

Uses:They causes miosis and contraction of the ciliary muscle
Decrease interocular pressure
Clinical: Used in open angle glaucoma
Problems: Has more topical adverse effects than any other antiglacoma drugs
Large doses may cause systemic toxicity
What are the characterizes of organophosphate poisoning?
Mechanism: muscarinic effects, nicotinic and CNS stimulations
Nicotinic blockade and CNS depression
Clinical signs: nausea, vomiting, diarrhea, coilic, salivation, miosis, urintation, muscle fasciculation, temors, repiratory failure


Treat with atropine 2-PAM (cholinesterase reactivator)
What is Atropine?
Classification:parasymathetolytic, antichoninergics, cholinoceptor-blocking drug) atropine is a tertiary antimuscarinic
Mechanism: competitive antagonist to Ach on muscarinic receptors
Clinical uses:
Eye: mydriasis increase IOP decreased lacrimation
Resp: bronchodilation and reducing secretion from the nose, decreases mucociliary clearance
Cardio: tachcardia vasconstriction
Urinary bladder: relaxation of wall of the gall bladder and contraction of the sphincter
GI: decrease GI motility
CNS: weak stimulation, blurred vision, mydriasis and cycloplegia (eye muscle paralysis)
Problems: causes tachycardia
Pharmacokinetics: admimistered PO, IV, IM and SC, readily absorbed wide distribution
Metabolized in the liver and excreted in urine and milk

USE IN INCOMPLETE AV BLOCK
What is Scopolamine?
A tertiary antimuscarinic that produces CNS depression
Used in motion sickness
Used as an ophthalmic agents to induce cycloplegia and for iritus and uveitis
What is Dicyclomine?
A tertiary antimuscarinic that has less systemic side effects tha atropine and is an antispasmodic
What is Aminopentamide?
A tertiary antimuscarinic that is approved as an antispasmodic and to treat GT spasm in dogs and cats
Available PO,IM and SC
What is Oxybutynin?
A tertiary antimuscarinic that is approved as adjunctive therapy for detrusor hyperreflexia in dogs and cats
What is Glycopyrroate?
A tertiary antimuscarinic that is more potent than atropine and antispasmodic, inhibits secretions
Less potent than atropine on cardio
Used as preanesthetic, bronchodilator and GI antispasmodic
Longer duration than atropine
What is propantheline?
A tertiary antimuscarinic that also blocks nicotinic receptors
Used as a GU antispasmodic agent and for urinary incintinence (neurogenic bladder)

Should not be used in patients with myasthenia gravis
What is Ipratropium?
A tertiary antimuscarinic that is more potent than atropine as a bronchodilator and less potent than a beta 2 agonist
Does not alter mucociliary clearance
Causes much less decrease in salivary secretion than atropine
Can be used with albuterol as a bronchodilatory and used intranasally for rhinitis
What are examples of catecholamine sympathomimetics?
Epinephrine
Norepinephrine
Isoproterenol
Dopamine
Dobutamine
What is Epinephine?
Classification: catecholamine sympathomimetics
Mechanism: a potent agonist of alpha 1 and 2 and beta 1 and 2 receptors
Stimulation of Beta receptors increases cAMP while stimulation of alpha decreases cAMP
Clinical uses: used for acute anaphylatic shock, bronchospasm, cardiac arrest, vasoconstrictor in surgical bleeding and combined with local anesthetics
Problems: can't used in closed angle glaucoma, hypertension, DM, phenothiazine overdose
Can causes sinus tachycardia, angina, hpertension, metabolic acidosis CNS stimulation
Pharmacokinetics: administered topically, inhalation, IM, SC, IV

USE IN COMPLETE AV BLOCK
What are the pharmacological effects of epinephrine on the eye?
Mydriasis alpha 1
Cycloplegia beta 2
Lowers interocular pressure in patients with open angle glaucoma
What are the pharmacological effects of epinephrine on the respiratory tract?
Bronchodilation and stabilization of mast cells (beta 2)
Increased mucociliary clearance
Decrease in bronchial secretion and decongestant effect
What are the pharmacological effects of epinephrine on the cardiovascular system?
Increase cardiac automaticity
Increased systolic pressure
Arteriolar vasconstriction a1 and a2 in blood vessels in the skin, subcutaneous and viscera and arteriolar vasodilation (b2) in blood vessles in skeletal muscles and coronaries
Low doses diastolic pressure decreases while at higher doses diastolic pressure increases
What are the pharmological effects of epinephrine on metabolism?
Hyperglycemia due to increased glycogenolysis (b2)
Hyperglycemia die to gluconeogenesis and inhibition of insulin release (a2)
Lipolysis of TG increase free fatty acids
What is norepinephrine?
catecholamine sympathomimetic that acts as an alpha and beta 1 adrenergic agonist
Increase both systolic and diastolic pressure
Causes less increase in myocardial O2 consumption than epinephrine
Increase peripheral resistance can cause reflex bradycardia
Used in intravenous infusion for septic and cardiogenic shock and hypotension
What is isoproterenol?
A synthetic sympathomimetic amine
A potent beta 1 and 2 agonist

Used by inhalation for brochial asthma and parenterally as a cardiac stimulant and bronchodilator
What is Dopamine?
Acts as an agonist of dopaminergic receptors and beta 1 and alpha adrenergic receptors and indirectly stimulating the release of norephinephrine
Dopaminergic receptors are the most senestive, than B1 and last are alpha receptors

Causes vasodilation and increase GFR is the most useful effect in conditions with decrease renal perfusion
Used by IV for:
Cardiogenic and septic shock
Congestive heart failure
Oliguric renal failure
To correct hypotenstion due to inhalation anesthetics
What is Epherdrine?
Alkaloid from Ephedra plant
A noncatecholamine that directly acts as adrenergic agonist on alpha and beta receptors and indirectly by releasing norepinephrine

Generally, it has similar pharmacological effects as epinephine and also stimulates the CNS

Has a slower onset and longer duration of action than epinephrine
Used topically

Continuous use causes tachyphylaxis
What is Amphetamine?
Indirect acting sympathomimetic

Acts by stimulating release of norepinephrine
What is Cocaine?
Indirect acting sympathomimetic

Acts by interfering with the reuptake or norepinephrine

has CNS stimulation

local anesthetic by blocking NA channels
CNS stimulation by inhibiting norepi
What are monamine oxidase inhibitors?
Used as anti depresssants that interfere

MAOI
What are alpha 1 selective agonists?
Phenylephrine
Methoxamine

Direct active non catecholamines
What is Phenylephrine?
Alpha one agonist
Used as decongestant for nasal and eye congestion
Used parenterally to increase BP and treat paroxysmal superventricular tachycardia
What are beta 2 selective agonists?
More selective in stimulating b2 than b1
B2 causes bronchodilation and stabilization of mast cells and increase mucociliary clearance
Increase cardiac stimulation, vasolation, uterine relaxation and hyperglycemia

Causes moderate hypokalemia by stimulating Na/k


Salmeterol
Albuterol
Terbutaline
Metaproterenol
Clenbuterol
Isoxuprine- not used as broncho dilation

know this order of drugs
What are sympatholytic (adrenoceptor antagonists)?
Direct acting (can be selective and non selective)
Alpha blockers
Beta blockers
Beta and alpha one blockers
What are alpha blockers?
Sympatholytic, can be nonselective and selective

Nonselective = phentoamine and phenoxybenzamine
Used for detrusor areflexia in dogs and cats
Hypertension due to pheochromocytoma in dogs

Prazosin = alpha 1 selective blockers
What are Beta blockers?
Sympatholytic

Nonselective = propranolol, timolol, sotalol

Beta 1 selective blockers
Atenolol
What are beta and alpha one blockers?
Sympatholytic

Carvedilol (drug example)

Antioxidant
Inhibits endothelin (ET) release
What is the mechanism of action and pharmacological effects of nonselective beta blockers?
Act as competetive beta 1 and 2 antagoinsts

Decreases heart rate and cardiac output and decreases in systolic pressure and myocardial O2 demand

Eye lower IOP by reducing the volume

Respiratory bronchoconstriction in bronchial asthma

Metabolic - hypoglycemia by inhibiting glycogenolysis (b2)

Urinary system decreased renal blood flow and GFR
What are the pharmacokinetics of nonselective beta blockers?
Administered as opthalmic agents, orally and parenterally
High lipid soluble
Readlily absorbed orally and cross the BBB
Duration of action is several hours
Metabolized in the liver and excreted in the urine
What are the therapeutic uses of nonselective beta blockers?
Glaucoma
Supraventricular and ventricular tacharrythmias
Myocardial hypertrophy
Hyperthyroidism
Hypertension

Congestive heart failure due to dilated cardiomyopathy
What are the adverse effects of non selective beta blockers?
Sudden withdrawal causes tachycardia (up regulation of b1)
Sinus bradycardia (AV block and can be treated with atropine, epinephrine, isoproterenol or glucagon)
Hypotention
Bronchospasm
Hypoglycemia
Hyperkalemia
Hypertriglyceridemia
sedation
What are beta 1 selective blockers used for?
Preferred in patients with bronchial asthma
Peripheral vascular occlusive disease
Diabetes mellitus


Effective in decreasing peripheral resistance than nonselecive beta blockers
What are muscle relaxants?
drugs that cause muscle relaxation centrally or peripherally and have an unknown mechanism of actions

drugs such as:
Guafenesin
Methocarbamol
What are the clinical uses for muscle relaxants (Guanfensin)
approved in horses but also used in cattle
as part of an anesthetic protocol what facilitates intubation, smooth induction and recovery and anesthetic sparing affect
possible expectorant in horses
What are the drug interactions with muscle relaxants (guafenesin)?
triple dipe
guafenesin + xylazine or detomindine + ketamine
thiopental
Physotigmine
What are precautions to take when using muscle relaxants (guafensin)?
Thombophlebitis with 10% soln
hemolysis with less than 10% in cattle give at 5%
precipitates out of solution at 22C or cooler
extralabel use in food animals (3days in meat, 48 hours in milk)
What is Methocarbamol?
muscle relaxant approved for dogs, cats and horses

Given IV and PO in dogs and cats and IV in horses
Carbamate of guafenesin not metabolized to guafenesin
Unknown mechanism of action
What are the clinical uses of Methocarbamol?
adjunct for treating acute inflammatory and traumatic conditions of the skeletal muscle
to reduce muscular spasms

In intervertebral disk disease
Urethral onstruction
Urinary retention

Strychnine, metadehyde, tetanus, permethrin toxicosis
What are the precautions/contradictions of Methocarbamol?
Sedation
Salivation
Emesis
Dark urine
What are examples of peripheral sites of action?
Motor neuron
NMJ
Muscle cell
What is Dantrolene?
A muscle relaxant
Ryanodine receptor antagonist
Inhibits Ca2 release from the sarcoplasmic reticulum
Used in the treatment of malignant hyperthermia, functional urethral obstruction, post anesthetic mitosytis, exertional rhabdomyolysis
What are neuromuscular blockers?
Drugs that causes paralysis in skeletal muscle. Must be used only when animals are unconscious before used, they must be ventilated.
NMB are used to perform tracheal intubation and institute artificial respiration.

Drug not to be used for beginners
What are the different types of neuromuscular blockers?
Depolarizing (noncompetitive) blockers

Nondepolarizing (competitive) blockers
What is Succinylcholine?
A depolarizing blocker
What is a phase I block?
Activation of nicotinic Ach receptors induces prolonged depolarization of the motor end plate
No complete repolarization prevents stimulation by Ach (depolarizing block)
What is phase II block
Nicotinic Ach receptors in inactivated state are unable to respond to Ach
What are the pharmacokinetics of depolarizing blockers?
Given IV and rarely IM
Hydrolization by plasma pseudocholinersterases
Succinylcholine-succinlmonocholine-succinic and choline
Acts in one circulation time duration of action 2-3min (20 min in dogs and ruminants)

Causes transient asynchronous muscle twitching followed by flaccid paralysis

Causes nicotinic Ach receptors at autonomic ganglia are less sensitive than those at the NMJ
Ganglionic stimulation - hypertension

Cardiovascular
Transient bradycardia
Hypertension (in unanesthetized animals)
Increased arrhythmogenicity to epinephine in halothane-anesthetized patients
Increased susceptibility of the heart to the action of digitalis preparations
Ocular - increased intraocural pressure due to contraction of ocular muscles

Serum potassium -hyperkalemia due to K release from skeletal muscles
,What are the uses of depolarizing blockers?
Facilitation of endotracheal intubation
Crash induction technique in dogs and cats
Prevenents laryngeal spam is cagt
To intubate pig and rabbits

Muscle relatation during surgery (rarely)
C-section in dogs

Adjunct to general anesthetics
No longer used (thiopental and succinylcholine in horses)
What are the adverse effects of depolarizing neuromuscular blockers?
Apnea - artificial respiration
Muscle fiber damage - increased creatine kinase, postop muscle pain
Hyperkalemia
Bradycardia
Increased arrhymogenicity to catecholamines
Malignant hyperthermia in susceptible animal
How do you reverse neuromuscular blockers?
Reversal is usually not needed, especially in dogs but you can provide artificial respiration
What are the precautions and contraindications of neuromuscular blockers?
Keep refrigerated to avoid spontaneous hydrolysis
Cholineresterase inhibitors
Glaucoma
Cardiac disease
What are the drug interactions for neuromuscular blockers?
Aminoglycosides
Magnesium salts
Local anesthetics
Cholinesterase inhibitors
Centrally-acting muscle relaxants
Digitalis preparations
What are some examples of Competitive neuromuscular blockers?
Pancurorium
Atracurium
Vecuronium
Mivacurium
Rocuronium
What is the mechanism of action of competitive neuromuscular blockers?
Competitive antagonism with Ach for nicotinic receptors at the motor end plate
What are the pharmacokinetic of competitive neuromuscular blockers?
Given IV (rarely IM)
Poor penetrators of membranes
Inactivated by plasma esterases
Metabolized in the liver
Excreted in bile
Excreted by the kidneys
What are the pharmacological effects of competitive neuromuscular blockers?
Skeletal muscle - flaccid paralysis
Autonomic- nicotinic Ach receptors at autonomic ganglia and less sensitive that those at the NMJ
Ganglionic blockade = hypotension
Cardiovascular- transient tachycardia (in anesthetized animals)
Weak hypotension

Histamine release - only with tubocurarine (increases increased respiratory tract secretions, bronchospasm hypotension)
What are the clinical uses of competitive neuromuscular blockers?
Facilitation of endotracheal intubation
Thoracic/upper abdominal surgery
Facilitate orthopedic manipulation
What are the adverse effects of competitive neuromuscular blockers?
Apnea
Histamine release
hypotension
How do you reverse competitive neuromuscular blockers?
Artificial respiration

Cholinesterase inhibitors (atropine or glycopyrrolate)
What are the precautions of competitive neuromuscular blockers?
Brochospasm
Hypotension
Liver or kidney disease
What are the drug interactions of competitive neuromuscular blockers?
Inhalation anesthetics
Aminoglycosides
Magnesium salts
Local anesthetics
Centrally acting muscle relaxants
Cholinesterase inhibitors
What is pulmonary edema
Fluid in the lungs and causes hypoxia, cyanosis, unconsciousness and death
What do you do to treat pulmonary edema?
Furosemide
Oxygen (give air breaks)
Inotropic agents - L ventricular failure
Colloids - correct hypoalbuminemia
Morphine - decrease RR and anxiety
Bronchodilators
Antibiotics corticosteroids
What are the problems seen with upper respiratory tract infections?
Inflammed mucus membranes
Excessive mucus production
Thick mucus
coughing
What do you see with Bronchitis?
Inflammed mucus membranes
Excessive mucus production
Thick mucus coughing
Cilia not working
Airway hyperreactivity
What do you see in patients with pneumonia?
hypoxia
How do you treat respiratory problems?
Treat primary problem
Many respiratory infections caused by viruses

Symptomatic treatment of secondary problem
What are expectorants?
Mucokinetics that:
Increase amounts of mucus
Decrease viscosity of mucus
Increase ciliary action
Cough up mucus
What are examples of mucolytic expectorants?
Not used much in vet med
Acetylcysteine
Carbocysteine
Bromhexine
What are cilia augmentors?
Increase beat frequency of airway cilia - functional mucociliary escalator system
Expectorants

Expectorants = KI AlCl
B2 agonists = Turbutaline, clenbuterol, albuterol
Methylxanthines = theophylline, aminophylline
What are antitussives?
drugs that reduce coughing
use in unproductive coughing
local anesthetic = lidocaine, benzonatate
opiods = butorphanol, hydrocodone, tramadol
bronchodilators
What are bronchodilators?
Reverse bronchoconstriction in cats and horses (used most often)


Used to help in asthma
What are examples of bronchodilators?
Sympathomimetics
A1 agonists - pseudoephedrine
B2 agonist tubutaline, clenbuterol, albuterol
Methylxantines = theophylline, animophylline
Anticolinergics = atropine, glycopyrrolate, ipratropium
Glucocorticoids= betamethasome, dexmethasone
What are methylxanthines?
a type of bronchodilator medication that act by nonselective inhibition of adenosine receptors

A1 decreases HR
A2a coronary artery vasocilation
A2b bronchonstriction
A3 inhibition of neutrophil degranulation
What are the pharmocological effects of Methylxanthines?
mild positive ionotropic
vasodilations
see tachycardia
mild diruetic activity
CNS stimulation
What are the pharmacokinetics of methylxanthines?
given orally
metabolized in the liver
metabolites excreted in the urine
What is Theophylline?
a methylxanthine
a bronchodilator used in dogs and cats
not useful in horese (toxic) or cattle (no effect)
What is pentoxifylline?
a methylxanthine but has no effect on respiratory pharmacology
used in horses for laminitis and navicular disease
What are the side effects of Methyxanthines?
vomiting
tachycardia
Diuresis
CNS stimulation at high doses
What do you see in Methylxanthine toxicity?
Acute onset short duration
Clinical signs the same as side effects
Bloodwork is non specific
Need to gastric lavage, induce vomiting or give activated charcoal
Antoconvulsants, antiarrhythimics, fluids, oxygen

Good prognosis if no major complications
What is Doxapram?
A respiratory stimulant
stimulates the CNS
Increases minute volume