Pharm Midterm3

Question 1

Glucocorticoids

Answer 1

These drugs are used in veterinary medicine to treat inflammatory, pruritic and immune-mediated disease as well as shock, laminitis, and adrenal insufficiency.
- Anti-inflammatories that can block the enzyme phospholipase and stop the inflammatory cascade that produces the formation of prostaglandin, which is a primary mediator of the immune response. These drugs also protect cells by stabilizing cell membranes to prevent their breakdown, including mast cells that produce histamine.
- Side effects of drugs in this category include polyuria, polydipsia, polyphagia, gastric ulcers, thinning of skin, muscle wasting and suppressed healing. Long-term use can result in a condition known as iatrogenic Cushing’s disease (hyperadrenocorticism).
- Safe use of anti-inflammatory drugs in this category includes applying topical formulations locally if possible, using the lowest dose/alternate-day dosing and tapering off slowly to prevent iatrogenic Addison’s disease hypoadrenocorticism.

Question 2

Acetate, Diacetate, Pivalate, Valerate

Answer 2

Ingredients associated with corticosteroid drug preparations that would identify the product as a suspension form, and therefore cannot be used by the IV route of administration.

Question 3

Prednisone

Answer 3

Glucocorticoid that must be converted to prednisolone by the liver, which is the active form of this drug. Therefore, animals with liver dysfunction should be prescribed prednisolone.

Question 4

NSAIDs

Answer 4

• This category of anti-inflammatory drugs work by either completely or selectively inhibiting cyclooxygenase (COX), which has two forms: cyclooxygenase-1 (COX-1) or cyclooxygenase-2 (COX-2).
• These drugs are commonly used in veterinary medicine mainly for post-operative pain, osteoarthritis and fever reduction.
• This group of anti-inflammatory drugs tend to have fewer side effects than glucocorticoids and produce analgesia, inhibition of platelet aggregation and fever reduction, which is not true of glucocorticoid drugs. Side effects include gastric ulceration, bleeding tendency, bone marrow suppression, and kidney and liver dysfunction.
• Anti-inflammatory drugs that are also referred to as prostaglandin inhibitors because they inhibit cyclooxygenase (COX) which is the enzyme that converts arachidonic acid to prostaglandin. The most common side effects associated with use of these drugs are gastric ulceration and bleeding tendencies.

Question 5

Acetylsalicylic Acid

Answer 5

(aspirin)
The oldest member of anti-inflammatory agents that is the representative of the salicylate category and a potent inhibitor of prostaglandin synthesis by COX inhibition. Cats cannot metabolize this drug as rapidly as other species due to deficiency of the glucuronyl transferase enzyme needed for metabolism. It is used most in veterinary medicine for post-adulticide treatment of heartworm disease to reduce platelet clumping associated with narrowed pulmonary arteries.

Question 6

Phenylbutazone

Answer 6

• Representative drug in the Pyrazolone category that is an inhibitor of prostaglandin synthesis by COX inhibition. This drug is frequently used in equine medicine for pain associated with the musculoskeletal system and is commonly referred to as “bute” by horse owners. Due to being highly protein bound and metabolized by the liver care must be taken if an animal has low albumin levels. Side effects include GI ulceration, diarrhea and renal necrosis, especially if given long-term in high doses.
• NSAID commonly used for musculoskeletal pain in horses that comes in paste, tablet, powder, gel and injectable forms. “Bute” has analgesic, anti-inflammatory and antipyretic action. The injectable form must be administered IV and if given perivascularly can result in skin necrosis and sloughing of tissues.

Question 7

Propionic Acid Derivatives

Answer 7

Also known as the “fen” group of NSAIDs which includes ibuprofen, ketoprofen, carprofen, and naproxen. Carprofen is believed to target COX-2 which acts only in stopping inflammation, and spares the protective GI prostaglandins, therefore having limited GI side effects. Although commonly used for pain and osteoarthritis in dogs, rare liver toxicity to carprofen has been noted (especially in Labrador retrievers), so it is recommended that liver enzymes are assessed prior to therapy.

Question 8

Lipooxygenase

Answer 8

Enzyme in the inflammatory pathway responsible for the formation of leukotrienes resulting in increased vascular permeability and WBC migration.

Question 9

Thromboxane

Answer 9

Product of the inflammatory pathway responsible for platelet aggregation and constriction of arterial smooth muscle.

Question 10

Prostaglandin

Answer 10

Mediator of inflammation that influences vascular permeability and vasodilation resulting in swelling, heat, redness and pain. This hormone like lipid compound is also responsible for maintaining health of the GI tract and blood supply to the kidney.

Question 11

Etodolac

Answer 11

An indol acetic acid derivative labeled as an anti-inflammatory and analgesic for osteoarthritis in dogs. Sometimes referred to as “aspirin” for dogs, it is believed to be a more selective inhibitor of COX-2 than COX-1 and therefore is more GI and kidney protective.

Question 12

Flunixin meglumine

Answer 12

This NSAID is a very potent analgesic, antipyretic and anti-inflammatory drug that works by COX inhibition. It is used extensively for pain associated with colic due to its ability to inhibit deep visceral pain and is also used for musculoskeletal disease in horses. Other uses include treatment of shock, post-operative pain and intervertebral disc disease. Although still labeled for both IV and IM injection, most equine clinicians avoid IM use due to risk of Clostridial infection. It’s also commonly called by its popular trade name “Banamine.”

Question 13

Selective COX-2 Inhibitors

Answer 13

The newest NSAIDS on the market that were developed to be more selective in their inhibition of inflammatory prostaglandins by targeting COX-2 to a greater degree than the GI and kidney protective COX-1 prostaglandins when administered at their recommended doses. Members of this group have “cox” or “lox” in their generic names and include deracoxib, firocoxib, robenacoxib and meloxicam.

Question 14

Meclofenamic acid

Answer 14

Representative drug of the fenamate group, this COX inhibitor is used as an analgesic and anti-inflammatory for osteoarthritis in horses. It comes in a granular form that is mixed in with feed.

Question 15

Diclofenac Sodium

Answer 15

A non-specific COX inhibitor that may also have some lipoxygenase inhibition. It is available as a topical cream for local control of joint pain and inflammation in horses. Clients should be warned to wear gloves when applying this product since it is absorbed across the skin.

Question 16

Dimethyl Sulfoxide

Answer 16

(DMSO)
Anti-inflammatory labeled for topically application to reduce acute swelling from trauma or other inflammatory conditions such as lick granulomas and constricted ear canals. It also acts as a carrier of other agents through the skin. Clients should wear gloves when applying this product since it can cause skin irritation/burning sensation, garlic smell/taste and birth defects.

Question 17

Grapiprant

Answer 17

The newest non-steroidal, non-COX inhibiting anti-inflammatory drug used for pain and inflammation associated with osteoarthritis in dogs 9 months of age or older and weighing greater than 8 pounds. It works by selectively inhibiting specific EP4 prostaglandin receptors and suppressing pain while reducing the GI, kidney and blood clotting effects seen with other anti-inflammatories that inhibit prostaglandins.

Question 18

Polysulfated Glycosaminoglycans

Answer 18

(PSGAGs) Semisynthetic product derived from bovine cartilage used for adjunct therapy of degenerative joint disease. This agent inhibits proteolytic enzymes that cause degeneration of joints and promotes production of joint fluid from the synovial membrane. It’s approved for IM injection in horses and dogs and one of the common trade names for this product is “Adequan.” Adverse effects are minimal.

Question 19

Hyaluronate Sodium

Answer 19

High viscosity mucopolysaccharide that mimics the composition of joint fluid and acts as a lubricant. It is used mainly for treatment of osteoarthritis in horse. It’s administered intra-articular to help cushion degenerating joints but can also be given intravenously. One of the common trade names for this product is “Legend.” Adverse effects are minimal.

Question 20

Nutraceuticals

Answer 20

Any nontoxic food component that has scientifically proven health benefits. Nutraceutical medicine involves the use of micro and macronutrients and other nutritional supplements as therapeutic agents.

Question 21

Chondroprotectives

Answer 21

Substances that can decrease the progression of osteoarthritis by providing support to cartilage and promoting its repair.

Question 22

Glucosamine and Chondroiten Sulfate

Answer 22

These products are believed to help the maintenance of cartilage structure and function by helping stimulate cartilage cell growth and maintaining cartilage strength and resilience. Typically used for adjunct therapy of osteoarthritis and degenerative joint disease, they are often one of the ingredients found in combination “joint supplements.”

Question 23

Methyl Sulfonyl Methane

Answer 23

(MSM) Dietary supplement form of sulfur that supports healthy connective tissue such as tendons, ligaments, and muscles. This product is seen in many combination joint supplements used for adjunct arthritis therapy.

Question 24

Acetaminophen (Tylenol)

Answer 24

Non-narcotic analgesic (NOT an NSAID) that has limited antipyretic and anti-inflammatory effects. It is rarely used in veterinary medicine due to toxic adverse effects. It is contraindicated in cats at any dosage due to their limited ability to metabolize the drug by the liver. Toxic metabolites build up and cause anemia, cyanosis, liver damage and lethal methemoglobinemia. Clients should be warned that it is toxic to animals!

Question 25

Redness, Heat, Swelling, and Pain

Answer 25

The four clinical manifestations or “cardinal signs” of inflammation.

Question 26

Antihistamines

Answer 26

Substances that are used to block the effects of histamine released from ruptured mast cells as a result of allergic or inflammatory process. They do not inhibit the formation of prostaglandins. The three most used in veterinary medicine are diphenhydramine, chlorpheniramine, and hydroxyzine. Have been shown to decrease steroid dose by as much as 50% when used in combination therapy. Adverse effects include drowsiness, dry mucous membranes, decreased GI secretions, and CNS stimulation in high doses.

Question 27

Analgesics

Answer 27

An agent that effects the loss of, or dissociation from pain. They work by stopping or preventing the perception of pain, the inflammatory process or the transmission of painful stimulus.

Question 28

Tranquilizers

Answer 28

A drug used to calm a patient by decreasing anxiety, not necessarily reducing awareness.

Question 29

Sedatives

Answer 29

A drug used to suppress brain activity and awareness with reduced excitement caused by sleepiness.

Question 30

Anticonvulsant

Answer 30

A drug used that inhibits seizure activity.

Question 31

Opioids

Answer 31

Opioids (or opiates) are derived from morphine and have many uses in veterinary medicine including pre-anesthesia, sedation, and analgesia. Members of this group are controlled substances and the level of control depends on the concentration of opioid in the product. Also known as “narcotics” this group includes morphine, oxymorphone, hydromorphone, fentanyl, butorphanol and buprenorphine. - This category of drugs can be used in multiple species and work by blocking the neurotransmission of pain to the brain and spinal cord receptors known as the Mu, Kappa, Delta and Sigma receptors. Most are Mu receptor agonists or partial agonists/antagonists and receptors are located in the CNS, smooth muscle, GI and urinary tracts. Analgesia is the major reasons for use of these drugs pre-intra-and post operatively and as part of neuroleptanalgesic anesthetic protocols. Other uses include cough suppression and as antidiarrheals.
- The major side effect of this group of drugs is respiratory depression, which is dose dependent and may be life threatening. Other adverse effects include bradycardia, hypotension, hypothermia/ hyperthermia (depending on species), diarrhea/vomiting initially, constipation with long term use, increased excitatory response to noise (especially cats), miosis/mydriasis (depending on species) and sweating (especially horses).

Question 32

Naloxone

Answer 32

Narcan, Competitive opioid antagonist that works by blocking opioids at the receptors and is used for reversal of opioid overdose. This reversal agent has a shorter duration of effect than the opioid itself and therefore may need repeat treatments until the patient is fully recovered.

Question 33

Fentanyl

Answer 33

Drug that is the most potent of the opioids and used primarily for severe orthopedic pain or end stage palliative cancer treatment in dogs and cats. It is available as a slow-release transdermal patch that may be applied to the dorsal neck after clipping/cleaning/drying the area. Clients should wear gloves when handling the patch to avoid accidental human exposure. The patch must never be cut or torn because this interferes with the rate of release and may lead to overdose. It is also administered IV, usually by constant rate of infusion, due to having a shorter duration of action in the injectable form.

Question 34

Butorphanol

Answer 34

Drug that is a C-IV opioid agonist/antagonist used for analgesia, cough suppression, and neuroleptanalgesia. It is commonly referred to as “torb” and was originally approved for cough suppression in dogs. There is less respiratory depression than other C-II and C-III opioids. This agent can also act as an opioid antagonist, but only has about 1/40 the reversal effect of naloxone.

Question 35

Buprenorphine

Answer 35

Drug that is a C-III opiate agonist/antagonist commonly used for pain control and can be effectively administered to cats orally in the mucosa of the buccal fold or sublingually. “Simbadol” is the trade name for the new FDA approved product labeled for cats, which can be administered SQ once daily for up to three days. There is less respiratory depression than C-II opioids.

Question 36

Tramadol

Answer 36

Drug that is a C-IV controlled “opioid-like” mild analgesic that’s an alternative to pure opioids and NSAID’s for analgesia. It can safely be used in conjunction with other analgesics and NSAID’s and therefore has gained popularity as an adjunct therapy for pain control.

Question 37

Phenobarbital

Answer 37

A long-acting C-IV barbiturate that depresses the motor centers of the cerebral cortex and is considered a first line drug of choice for maintenance anticonvulsant therapy. Phenobarbital is highly protein bound, and has a long half-life, taking 2-4 weeks to reach a stable blood level.
- Anticonvulsant barbiturate that undergoes “induced biotransformation” causing the rate of drug metabolism to be increased with continued use, also called the “tolerance” phenomenon. Therefore, a patient on phenobarbital should have regular blood evaluations, at least every 6 months, due to the potential for inadequate drug levels that may cause “breakthrough” seizures. Side effects typically include polyuria, polydipsia, polyphagia and liver enzyme elevation. Long term use may result in liver damage.

Question 38

Potassium bromide

Answer 38

(KBr)
A concentrated salt that works by stabilizing nerve cell membranes and is becoming more common as an anticonvulsant therapy used either alone or in conjunction with phenobarbital. It has an extremely long half-life and can take up to 4 months to have clinical effects, so is not the drug of choice for uncontrolled or frequently seizing patients.

Question 39

Benzodiazepines

Answer 39

Category of drugs that are similar in structure and mechanism of action. They are thought to bind with and promote GABA neurotransmitter activity in the cerebral cortex and limbic system, which inhibits impulse transmission in nerve cells. Members of this group include diazepam, midazolam, lorazepam, alprazolam and clonazepam and they are used in veterinary medicine for their anti-anxiety, anticonvulsant, sedative, analgesic and muscle relaxation properties. Adverse effects include lethargy, ataxia, polyuria/polydipsia, hyperexcitability and hepatic necrosis (especially in cats). Tolerance may develop and withdrawal signs may occur if benzodiazepines are stopped abruptly (varies between drugs).

Question 40

Diazepam

Answer 40

C-IV Benzodiazepine that is considered the drug of choice for emergency seizure therapy, and may be administered by the IV, intranasal or rectal routes of administration. It also is used IV as an appetite stimulant in cats. It has a short duration of action so is not the drug of choice for maintenance therapy of seizures. It is commonly referred to by the trade name “Valium.” Due to being light sensitive it should be stored in a dark location. The injectable solution absorbs to plastic materials and when given IV should be administered slowly because the propylene glycol carrier can cause bradycardia.

Question 41

Midazolam

Answer 41

C-IV benzodiazepine that has gained popularity as an anticonvulsant due to being more readily available today than diazepam. This drug has a shorter duration of action than diazepam and can be administered by the IV, IM and intranasal routes of administration. Unlike diazepam, this anticonvulsant drug is not effective when given by the rectal route.

Question 42

Levetiracetam

Answer 42

(Keppra)
Anticonvulsant that is not a controlled substance and is believed to work by selectively affecting the release of neurotransmitters and impeding impulse conduction across synapses. It is used IV for Status Epilepticus and as an adjunct for refractory seizure patients or when phenobarbital and/or potassium bromide is not well tolerated. It is being used more as a first line anticonvulsant, especially in young animals, and is well tolerated. Adverse effects may be transient and include sedation in dogs, and lethargy and decreased appetite in cats.

Question 43

Methylxanthines

Answer 43

Category of central nervous system stimulants used mainly for respiratory diseases requiring bronchodilation. Included in this group are aminophylline, theophylline, and the “theobromines” such as caffeine and chocolate, which can be toxic to animals. Adverse effects are usually dose related and include vomiting/diarrhea, tachyarrhythmias, CNS stimulation, tremors, and seizures.

Question 44

Doxapram

Answer 44

CNS stimulant that is used to increase respirations in animals due to anesthetic respiratory depression. It is also used to stimulate respiration in neonates following C-section by placing 1-2 drops sublingually or by injection into the umbilical vein. Caution should be used in animals with a history of seizures.

Question 45

Alpha-2-adrenergic Antagonists

Answer 45

Reversal agents for alpha-2-adrenergic agonists such as xylazine and dexmedetomidine that work by blocking alpha-2-adrenergic receptors allowing norepinephrine to be released. Member of this group include yohimbine and tolazoline (reverses xylazine) and atipamezole (reverses dexmedetomidine).

Question 46

Spasmolytics

Answer 46

Category of drugs used to treat acute episodes of muscle spasticity associated with various neurological and musculoskeletal disorders. Examples of drugs in this category include methocarbamol, guaifenesin, diazepam, and dantrolene.

Question 47

Methocarbamol

Answer 47

A potent skeletal muscle relaxant used as an adjunct treatment for inflammatory/traumatic skeletal muscle conditions such as intervertebral disc disease. This agent helps reduce muscle spasms but does not decrease muscle tone. Clients should be warned that this drug causes a brownish discoloration to the urine.

Question 48

Guaifenesin

Answer 48

(Mucinex)
This drug is a muscle relaxant that works on laryngeal/pharyngeal muscles and is commonly used in horses to aid intubation. It is also an expectorant that thins mucus secretions for the treatment of productive coughs.

Question 49

Dantrolene

Answer 49

This drug is a muscle relaxant used for the treatment of malignant hyperthermia in various species, postanesthetic myositis in horses, and after treatment of urinary obstruction in male cats due to reduction of urethral sphincter spasms.

Question 50

Tramadol

Answer 50

A C-IV controlled “opioid-like” analgesic that’s an alternative to pure opioids and NSAID’s. It can safely be used in conjunction with other analgesics and NSAID’s and therefore has gained popularity as an adjunctive therapy for post-operative or chronic pain control in dogs and horses.

Question 51

What is the difference between COX1 and COX2 ?

Answer 51

Cycoloxygenase-2 is believed to be more involved with inflammatory prostaglandins, whereas cyclooxygenase-1 is believed to be more involved with the protective stomach and kidney prostaglandins.