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PHARMACOLOGY REVIEWER MODULE 1

 Inflammation is a useful and normal process – Increase the risk of corneal ulceration if corneal
that consists of a series of events, destroy damage exists
harmful agents at the injury site and repair
– May induce abortion in some species
damaged tissue.
 5 cardinal signs of inflammation Corticosteroids are used to suppress the immune
o PAIN system in allergic conditions such as flea dermatitis,
o HEAT atopy, autoimmune hemolytic anemia, rheumatoid
o REDNESS arthritis, and uveitis.
o SWELLING
Corticosteroids are useful in the treatment of
o DECREASED RANGE OF MOTION
lymphoid tumors because they cause a direct
 Steroidal anti-inflammatory drugs block the
lymphotoxic effect.
action of phospholipase
 Nonsteroidal anti-inflammatory drugs block Steroids are formed in three regions of the adrenal
the action of cyclooxygenase gland.
 Glucocorticoids as drugs
1. Zona glomerulosa –mineralocorticoids
o Betamethasone
o Cortisone 2. Zona fasciculate – glucocorticoids
o Dexamethasone
3. Zona reticularis – sex hormones (androgen &
o Fluprednisolone
estrogen
o Hydrocortisone
o Meprednisone NON-STEROIDAL ANTI-INFLAMMATORY
o Methylprenisone DRUGS
o Prednisolone
Common mechanism shared by NSAIDs: inhibition
o Prenisone
of cyclooxygenase (COX) enzyme(s) Decreased synthesis
 Short-acting -Cortisone and hydrocortisone
of various prostaglandins and thromboxane
 Intermediate-acting-Prednisone, Prednisolone,
methylprednisolone, methylprednisolone Examples
acetate, and triamcinolone
 Long-acting -Dexamethasone, betamethasone, Acetylated carboxillic acids/salicylates
and fluocinolone o Aspirin
 GLUCOCORTICOID USES o Meclofenamic acid
– Reduce inflammation and pain o Flunixin meglumine

– Relieve pruritus Non-acetylated carboxillic acid

– Reduce scarring by delaying wound healing o Magnesium salicylate,

o Salicylamide,
– Reduce tissue damage
o Sodium salicylate
Drawbacks:
Acetic acids
– Delay wound healing
o Diclofenac,
– Increase risk of infection o Etodolac
– May cause GI ulceration and bleeding Propionic acids

o Ibuprofen,

o Naproxen,
o Ketoprofen*,
o Carprofen*,
Fenamic acids
o Mefenamic acid,
o meclofenamic acid
Enolic acids
o Oxyphenbutasone,
o Phenylbutazone*,
o Piroxicam*,
o Dipyrone
o Meloxicam
Non-acidilic
o Nabumetone
Recommmend NSAIDs
 Flunixin (at the labeled dosage) is generally
considered a powerful analgesic but it is only
used for short durations.
 Phenylbutazone (at generally accepted dosage)
is only modest analgesic. Higher doses are
analgesic but can only be used for short
duration.
 Aspirin is usually dosed for mild to moderate
activity. Higher doses are more analgesic but
can only be used for short durations
Toxicity
1. Gatrointestinal - primarily due to inhibition of
PGE2 activity ( mediates local increase in blood
flow and maturation of gastric lining cells).
2. Renal – toxicity results from interruption of
prostaglandin mediated regulation of blood
flow
3. Coagulation – a desirable effect in some
situations but can be a problem. This effect is
mediated by the elimination of TXB2
(thromboxane) synthesis by the platelets
thereby decreasing ability to adhere.Aspirin
4. Allergy - bronchospasm and urticaria reported
with NSAIDs; increase synthesis of leukotrienes
by lipoxygenase
2
5. Hepatotoxicity – possible with ALL NSAIDs. This
effect with carprofen should not have been a
surprise
6. Blood dyscrasia – phenylbutazone. This makes
extra – label use in food animals questionable
(blood dyscrasia’s in people consuming meat).
7. Reproductive system - some concern over
effect on male fertility.
INDIVIDUAL NSAIDS
Aspirin
 In the cat, aspirin is probably still safest NSAIDs.
It must be still be dosed with care
 Analgesic in the dog, cat, cattle
 In the dog, aspirin has largely replaced by
carporfen and etodolac
 Antipyretic in cats and cattle.
 Most frequent use to prevent “saddle
thrombus” in cats with cardiomyopathy.
 Postadulticide treatment for heartworm
disease
 Treatment of endotoxic shock
 Enteric-coated aspirin, such as Ecotrin, may be
used to prevent gastric irritation.
Phenylbutazone
 A pyrazolone derivative is an NSAID
 Analgesia for mild to moderate pain
 Anti-inflammatory action
 Antipyrexia
 Musculoskeletal pain/inflammation (dominant
use)
 Almost exclusively for horse
 Phenylbutazone injection should be
administered by the intravenous route only
 possible bone marrow suppression and
potential ulcer formation, animals that are
receiving long-term treatment with
phenybutazone.
Flunixin meglumine (Banamine)
 It is labeled for use in horses and cattle

 Analgesia
 Anti-inflammatory action
 Antipyrexia
 In horses include alleviation of pain associated
with musculoskeletal disorders and colic.
(Flunixin apparently has great ability to inhibit
visceral pain)
INCLUDE TREAMENT IN THE FOLLOWING
1. Disk disease
2. Endotoxic shock
3. Calf diarrhea
4. Parvovirus disease
5. Heatstroke
6. Opththalmic conditions
7. Postsurgical pain
Dimethyl Sulfoxide (DMSO)
 ability to act as a carrier of other agents through
the skin.
 DMSO causes vasodilation when applied
topically.
 An adjunct to intestinal surgery (intravenously)
 A treatment for cerebral edema or spinal cord
injury (intravenously)
 A treatment for perivascular injection of
chemotherapeutic agents or other irritating
substances (topical).
 A carrier of drugs across the skin.
Buscopan compositum
 For management of abdominal pain associated
with equine colic.
Acetaminophen (Paracetamol)
 It is an analgesic with limited antipyretic and
anti-inflammatory activities
 Acetaminophen should never be given to cats
Ketoprofen
 It is labeled for use in horses in the US but has
been used a great deal in dogs and cats in
Europe and Canada.
 In horses, it is used for treatment of pain and
inflammation associated with musculoskeletal
disorders. It has been used for postoperative
and chronic pain in dogs and cats.
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Naproxen
 It is similar to ketoprofen and ibuprofen. It is
labeled for use in horses, although it has been
used in dogs
 “relief of pain, inflammation and lameness
associated with myositis and other soft tissue
diseases of the musculoskeletal system of
horses.”
Ibuprofen
 it is reported to have potential for serious side
effects in dogs and cats and it is not
recommended for use in these species
Cox 2 SELECTIVE INHIBITORS COXIBS
Deracoxib (Deramaxx®)
 It is labeled for the control of pain and
inflammation associated with orthopedic
surgery in dogs with 4 lb body weight or
greater, and for the control of pain and
inflammation associated with osteoarthritis in
dogs weighing 14 lb or more.
Firocoxib
 treatment of pain
 inflammation associated with osteoarthritis in
dogs
Tepoxalin
 Dual inhibitor of COX and LOX. By inhibiting
both COX1 and COX2 and 5 LOX
 It is orally use in dogs. The manufacturer claims
that this product is the only NSAID that blocks
both arms of the arachidonic acid cascade (COX
and lipoxygenase). It is manufactured as a
rapidly disintegrating tablet that breaks down
quickly upon contact with the moisture of the
animal’s mouth and cannot be spit out
Meloxicam
 Metacam use in cats limited to one-time
subcutaneous injection for surgical pain.
 It is a COX-2 receptor NSAID. It has anti-
inflammatory, analgesic, and antipyretic
properties.
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 Meperidine,
 Methadone,
 Morphine,
 Oxymorphone,
 Sufentanil
Cats are more sensitive to the excitatory
MISCELLANEOUS ANTIINFLAMMATORY DRUGS effects of opiod agonists than are other
species, and they tolerate low doses well

Polysulfated Glycosaminoglycan (Adequan) (PSAG) Opioid Agonists-antagonists

 HORSE AND DOGS These drugs bind with opioid kappa receptors but
 A semisynthetic mixture of glycosaminoglycans antagonize opioid mu receptors.  These include
derived from bovine cartilage(trachea). butorphanol, pentazocine and nalbuphine.
 This drug reduces degenerative changes
induced by noninfectious or traumatic joint
disease and promotes activity in the synovial Opioid Partial Agonists
membrane
The opioid partial agonists bind with the mu receptor
Meclofenamic Acid (arquel Granules) but only partially activate them.  Buprenorphine is the
primary drug in this category
 For oral treatment of acute or chronic
inflammatory disease in horses

Selenium and Vitamin E (Seletoc) AUTOCOIDS

 For relief of acute symptoms of arthritic  play a key role in allergy, inflammation, smooth
conditions in dogs. muscle function, pain, and certain types of drug
reactions (anaphylaxis)
Ketorolac
 are chemical mediators that are synthesized
 With efficacy similar to that of morphine. It and function in a localized tissue or area and
carries a human lable and may cause serious participate in physiologic or pathologic
side effects responses to injury
 They act only locally and therefore also termed
Orgotein (Palossein)
“local hormone.”
 For acute and chronic inflammatory conditions
Antihistamines are used to treat the following:
in horses and pigs
 Pruritus
OPIOD AGONISTS  Urticaria angioedema associated with acute
These are used to control moderate to severe pain in allergic reactions
animals  laminitis in horses and cattle
 “Downer” cow syndrome
 Alfentanil,  motion sickness
 Carfentanil,  “Reverse sneeze’ syndrome
 Codeine,  Anaphylactic shock 8. Upper respiratory tract
 Etorphine, condition
 Fentanyl,
Histamine
 Hydromorphone,

 is widely distributed in tissues and its
concentration and rate of synthesis varies
greatly from tissue to tissue
Respiration
 is the exchange of gases between the
atmosphere and the cells of the body
Ventilation
 is the bringing in of fresh air
PRINCIPLES OF RESPIRATORY THERAPEUTICS
 CONTROL OF SECRETIONS
Secretions may be reduced by decreasing their
production or increasing their elimination.
 CONTROL OF REFLEXES
coughing may be suppressed through the use of
antitussives or bronchodilators if the cough is
nonproductive
 MAINTAINING NORMAL AIRFLOW TO THE
ALVEOLI
airflow to the alveoli maybe maintained by
reversing bronchoconstriction, by removing
edema or mucus from alveoli snd air passages,
and by providing oxygen therapy
INHALATION THERAPY FOR RESPIRATORY
DISEASE
 Aerosolization (nebulization)
of drugs allow their delivery at high
concentrations directly into the airways while
minimizing their blood levels- a feature they
may reduce the chance of toxic reaction.
CATEGORIES OF RESPIRATORY DRUGS
 EXPECTORANTS
Increase the flow of respiratory secretions to
allow material to be coughed up from the lungs
Increase the fluidity of mucus
 MUCOLYTICS
Decrease the viscosity or thickness of
respiratory secretions by altering the chemical
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composition of the mucus through the
breakdown of chemical (disulfide) bond
 ANTITUSSIVES
Suppress coughs
 BRONCHODILATORS
Widen the lumen of the bronchi and counteract
bronchoconstriction by 3 basic mechanisms:
o Release of ACH at parasympathetic
nerve endings or inhibition of
acetylcholinesterase
o Release of histamine through allergic or
inflammatory mechanisms
o Blockade of beta 2-adrenergic receptors
by drugs such as propanolol results in
bronchoconstriction
BASIC CATEGORIES OF BRONCHODILATORS
o CHOLINERGIC BLOCKERS
It produces bronchodilation by combining with
Ach receptors on smooth mm. fibers and
preventing the bronchoconstrictive effects of Ac
o ANTIHISTAMINES
Block the effects of histamine
Respiratory conditions that may be treated with
antihistamines includes “heaves” in horses,
pneumonia in cattle, feline asthma, and insect
bites.
It is used to treat allergic and respiratory
conditions. They may be used for their
antiemetic effects.
o BETA 2 ADRENERGICS
These drugs are combined with appropriate
receptors on the smooth mm. fibers and effect
relation of those fibe
r
o METHYLXANTHINES

Derivatives of these drugs are used
therapeutically include aminophylline and
theophylline.
inhibit an enzyme in smooth m. cells called
PHOSPHODIESTERASE
Caffeine and theobromine (found in chocolate)
are methylxanthine
Methylxanthines are used for bronchodilation in
respiratory and cardiac conditions and for mild
heart stimulation (positive inotropic effect)
DRUGS INDEX AND CATEGORIES
EXPECTORANTS
GUIAFENESIN (GLYCERYL GUAIACOLATE)
Commonly used in equine practice to induce or
maintain general anesthesia
Commonly used in equine practice to induce or
maintain general anesthesia
MUCOLYTICS
ACETYLCYSTEINE
also used to treat acetaminophen toxicity
It is used to break down thick inspissated
respiratory mucus
ANTITUSSIVES
BUTORPHANOL TARTRATE
Class IV controlled substance. It is also used as
preanesthetic and as an analgesic
Used for relief of chronic nonproductive cough
in dogs and analgesisa and preanesthesia in
dogs and cats.
HYDROCODONE BITARTRATE
A CLASS III opiate agonist used for the
treatment of nonproductive cough in dog
CODEINE
A schedule V opiate agonist that is used as an
antitussive in human label combination
products
DEXTROMETHORPHAN
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A non-narcotic antitussive that is chemically
similar to codeine. It has no analgesic or
addictive properties. It acts centrally and
elevates the cough threshold.
TEMARIL-P
Combination of centrally acting antitussive
(trimeprazine tartrate) & corticosteroid
(prednisolone).
BRONCHODILATORS
CHOLINERGIC BLOCKERS
Atropine, aminopentamide (Centrine), and
glycopyrrolate (Robinul-V) good in
organophospate or carbamate toxicity
Ipratropium bromide, a synthetic
anticholinergic, may be of some value in
treating equine pulmonary obstructive disease
BETA-2-ADRENERGIC AGONIST
Epinephrine. used only in life-threatening
situations (e.g. anaphylactic shock) because it
also produces significant tachycardia.
Isoproterenol (Isuprel).
Albuterol, clenbuterol terbutaline (Brethine)
and metaproterenol (Alupent).
Clenbuterol is veterinary approved for horses
and is not intended for food.
Ephedrine, Isopreterenol ,Noreipenephrine
METHYLXANTHINES
aminophylline and theophylline
inhibit an enzyme in smooth m. cells called
PHOSPHODIESTERASE.
Caffeine and theobromine (found in chocolate)
are methylxanthines
ANTIHISTAMINES
Block histamine
diphenhydramine and chlorpheniramine
DECONGESTANTS
Decrease the congestion of nasal passages by
reducing swelling

phenylephrine and pseudoephedrine,
ephedrine
CORTICOSTEROIDS
Used primarily to treat allergic respiratory
conditions. It is considered as the most effective
drugs in treatment of equine chronic
obstructive pulmonary disease
Used to treat equine heaves, feline asthma,
acute respiratory distress syndrome and allergic
pneumonia.
RESPIRATORY STIMULANTS
DOXAPRAM HCL
It is a general CNS stimulant that is used
primarily as a stimulant for the respiratory
system
It is used for stimulation of respiration during
and after anesthesia and to speed awakening
and restoration of reflexes after anesthesia. In
neonatal animals, doxapram is used to
stimulate respiration after dystocia or cesarean
section.
NALOXONE
o Stimulate respirations in narcotic overdose
YOBINE
o Is used to stimulate respirations in xylazine
overdose
VOLATILE OILS (terpine hydrate, eucalyptus, menthol,
pine oil
o directly stimulate the tubuloacinar glands
following absorption when administered orally
or when efficacy is lacking
Cardiovascular Drugs
• Heart rate is controlled primarily by the autonomic
nervous system:
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– Stimulation of the parasympathetic nervous system
slows heart rate
– Stimulation of the sympathetic nervous system
increases heart rate
Preload: volume of blood entering the right side of the
heart
Afterload: force needed to push blood out of the
ventricles.
TERMS:
ARRHYTHMIA (DYSRHYTHMIA) – a variation from the
normal rhythm.
AUTOMATICITY – the ability of cardiac muscle to
generate impulses.
BRADYARRYTHMIA – bradycardia associated with an
irregularity of heart rhythm.
BRADYCARDIA – a slower-than-normal heart rate.
CHRONOTROPIC – affecting the heart rate
DEPOLARIZATION – neutralizing of the polarity of
cardiac cell by an inflow of sodium ions. depolarization
results in contraction of the cardiac cell and renders it
incapable of further contraction until repolarization
occurs.
INOTROPIC – affecting the force of cardiac muscle
contraction
PREMATURE VENTRICULAR CONTRACTION (PVC) –
contraction of the ventricles without a corresponding
contraction of the atria, PVCs arise from an irritable
focus or foci in ventricles
REPOLARIZATION – the return of the cell membrane to
its resting polarity after depolarization
TACHYARRYTHMIA – tachycardia associated with an
irregularity in normal heart rhythm TACHYCARDIA – a
faster-than-normal heart rate.
COMPENSATORY MECHANISMS OF THE
CARDIOVASCULAR SYSTEM
 Increasing heart rate
 Increasing the stroke volume
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 Increasing the stroke volume BASIC OBJECTIVES IN THE TREATMENT OF

 Physiologic heart enlargement CARDIOVASCULAR DISEASE

1. Control rhythm disturbances

Many disorders can result in cardiac disease 2. Maintain or increase cardiac output

1. Valvular disease a. increase the strength of contraction

a backflow or leakage of blood backward b. decrease the afterload ( I ) Arteriolar dilator
through the valve, is a relatively common
acquired heart disorder of dogs. If the tricuspid c. Decrease the preload (I) venodilator
valve is affected, ascites may occur. If the mitral
3. Relieve fluid accumulations
valve is involved, pulmonary edema may result.
a. diuretics
2. Cardiac arrhythmias
b. dietary salt restriction
If a focus of cardiac tissue depolarizes out of
sequence with the sinoatrial node, an 4. Increase the oxygenation of the blood
arrhythmia may result. Various types of
a. bronchodilation
arrhythmias, including tachyarrhythmias and
bradyarrhythmias, may occur. 5. Ancillary treatment

a. narcotics/sedatives
3. Myocardial disease
Cardiomyopathy, is a disease of the b. oxygen
myocardium, primarily affects dogs and cats. It
may be classified as congestive (the
myocardium becomes thin and ineffective in its Cardiovascular Drugs
pumping action)
4. Other potential causes of cardiac disease Increasing or decreasing the force of myocardial
congenital defects (right-to-left shunts), contraction.
abnormalities of cardiac innervations, vascular ○ Positive inotropic drugs- increase the force of
disease (hypertension), and heartworm contraction.
disease
○ Negative inotropic drugs -reduce the force of
contraction
Stages and Treatment of Cardiac Disease ● Increasing or decreasing heart rate by altering the
rate of impulse formation at the SA node.

○ Positive chronotropic drugs - increase heart rate

○ Negative chronotropic drugs - decrease heart rate

● Increasing or decreasing the conduction of electrical

impulses through the myocardium.

○ Positive dromotropic drugs- increase the rate of

electrical conduction

○ Negative dromotropic drugs - decrease the rate of

electrical conduction

Positive inotropic drugs-Commonly used to increase
the strength of contractions by failing heart muscle
cardiac glycosides, catecholamines, & benzimidazole-
pyridazinones
 Cardiac Glycosides (Digitalis)- Derived from
dried leaves of the plant Digitalis purpurea
 Catecholamines-(increase blood pressure,
Elevate blood glucose levels.
 Epinephrine-Has both alpha and beta activity.
causes bronchodilation, raises blood glucose
levels, and increases heart rate and
contractility.
 Dopamine-Biosynthetic precursor of
norepinephrine .Increased heart contractility,
heart rate, and blood pressure and supportive
treatment of shock.
 Dobutamine-It is given as a constant-rate IV
infusion. increased cardiac output without the
dilation of blood vessels seen with dopamine
 Isoproterenol-treatment of cardiac arrhythmias
and bronchial constriction
BIPYRIDINE DERIVATIVES
Amrinone and milrinone work by inhibiting enzymes
that ultimately lead to an increase in cellular calcium
Amrinone (inocor) is given IV and is limited to short
term inpatient use
Milrinone is given orally and has potential for long-term
use.
ANTIARRHYTHMIC DRUGS
1. Decreasing automaticity
2. Altering the rate of electrical impulse conduction
3. Altering the refractory period of the heart muscle
between consecutive contractions
Classification Antiarrhythmic Drugs
1. Class IA includes quinidine, procainamide, and others
a. Class IB includes lidocaine, tocainide, and mexiletine.
b. Class IC includes flecainide and encainide.
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2. Class II includes the beta-adrenergic blockers
(propranolol).
3. Class III includes bretylium and miodarone.
4. Class IV includes the calcium channel blockers
(verapamil, nifedipine, amlodipine, and diltiazem
Class IA: Local Anesthetics
local anesthetics to the nerves and myocardial
membrane
 Quinidine
 Procainamide
Class IB: Membrane Stabilization
 This group works by blocking the influx of
sodium into the cell, thus stabilizing the
myocardium and preventing depolarization
(shortens the duration of the action
potential)
 lidocaine, tocainide, and mexiletine.
Class II: Beta-Adrenergic Blockers
 This group works by blocking beta-adrenergic
receptors or by preventing release of
norepinephrine from the adrenergic neuron
(depresses the depolarization phase)
 Propranolol
Class III: Potassium Channel Blockers
 This group works by lengthening the time
between action potentials, which decreases the
sinus rate
 bretylium and miodarone, sotalol
Class IV: Calcium Channel Blockers
 This group works by blocking channels that
allow calcium to enter the myocardial cell
 Verapamil, nifedipine, nifedipine
Vasodilator Drugs
 Vasodilators are drugs used to dilate arteries
and/or veins, which alleviates vessel
 10

constriction and improves cardiac output. The 4. Aspirin – it is used to reduce clot formation in the
actions of vasodilators often greatly improve heartworm treatment for the same purpose in
the condition of an animal with CHF. congestive cardiomyopahty in cats.
 Types:
5. Thoracocentesis and abdominocentesis – when
○ Angiotensin-Converting Enzyme Inhibitors
heart failure is accompanied by excessive fluid (effusion)
○ Arteriole Dilators
in the thoracic cavity, drawing fluid from the cavity may
○ Venodilators
be lifesaving. Removal of ascetic fluid is controversial
○ Combined Vasodilators
but may relieve pressure on the diaphragm and improve
○ Calcium Channel Blockers
ventilation.
Arteriole Dilators: Hydralazine

 used to reduce the afterload associated with

CHF.

Venodilators: Nitroglycerin ointment

 Used to improve cardiac output and reduce

pulmonary edema (small animals). ● It is
applied as a dose in inches to the skin.

Angiotensin-Converting Enzyme Inhibitors

 CE inhibitors are combined vasodilators (both

venous and arterial) used in the treatment of
heart failure and hypertension.
 They prevent the conversion of angiotensin I to
angiotensin II .

ANCILLARY TREATMENT OF HEART FAILURE

1. Bronchodilators such as aminophylline and

theophylline are sometimes used in the treatment of
heart failure

2. Oxygen therapy – animals with pulmonary edema

benefit greatly from the administration of 40% to 50%
oxygen via cage, mask, or nasal cannula.

3. Sedation – animals with pulmonary edema caused by

heart failure often experience a great deal of anxiety
because of the dyspnea that they encounter. This
anxiety often leads to hyperventilation and even greater
oxygen demant and anxiety. To break the cycle and
calm the animal, sedative drugs are often administered.
The clinician may choose morphine, meperidine,
diazepam or other drugs.