Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Veterinary Pharmacology > Midterm II - Topic 22-23 > Flashcards

Midterm II - Topic 22-23 Flashcards

22-23: NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

1
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

History

Salix Alba

A

Salix Alba:

Bad side effects of:

  • gastric ulceration,
  • blood vomiting (can be life threatening).

The revolution came from Felix Hoffmann (German). He found out how to synthesize aspirin from Salix Alba.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Drug group A inhibits PLA2 enzyme, While drug group B inhibits C enzyme, Therefore A, B and C are?

A

A= GLUCOCORTICOIDS

B= NSAID’s

C= Cyclooxygenase (COX)

Glucocorticoids inhibits PLA2 enzyme, While NSAIDs inhibits COX enzyme

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Eicosanoids = Aracidonic acid is the substrate for which enzymes?

A
  1. Apoxygenase,
  2. lipoxygenase
  3. cyclooxygenase.
  4. Apoxygenase and lipoxygenase have limited significance.
  5. Lipoxygenase produces leukotrienes and lipoxins which play an important role in asthma i.e. respiratory inflammation.

Therefore, lipoxygenase inhibitors are important in human medicine but are not used in veterinary medicine.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Eicosanoids = Arachidonic acid is the substrate for CYCLOOXYGEBASE enzyme, but why is it important?

A
  • They produce
    • prostaglandins (PGF and PGE),
    • prostacyclins (PGI), and
    • thromboxanes (TX).
  • These mediators will produce
    • pain,
    • edema, and
    • other signs of inflammation.
      • This is why we end up with inflammation when we have cellular damage e.g. cut on the skin.
      • The function of TX at the site of injury and inflammation is to cause aggregation of the platelets leading to blood clotting.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Eicosanoids = Arachidonic acid

How can we inhibit Phospholipase A2

A
  • Pharmacologically, we can inhibit phospholipase A2

= entire process will be inhibited.

  • These are the best anti-inflammatories and are known as GLUCOCORTICOIDS.
  • Most potent anti-inflammatories we know e.g.
    • PREDNISOLONE.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Eicosanoids = Arachidonic acid

How to inhibit COX enzyme and why?

A
  • With cyclooxygenase inhibitors are known as
    • NSAIDs.
  • These inhibit the function of cyclooxygenase.

COX is increasing inflammation and pain sensation, this phenomenon is known as peripheral sensitization.

This means that at the site of inflammation, we feel pain better or stronger.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is Peripheral sensitization phenomenon

A

COX is increasing inflammation and pain sensation, this phenomenon is known as peripheral sensitization.

This means that at the site of inflammation, we feel pain better or stronger.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

How many isoenzymes does the cox enzyme have in the body?

A

Cyclooxygenase has at least two isoenzymes in the body

  1. COX-1
  2. COX-2
  3. (COX-3)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the function of COX-1?

A

COX-1:

This is the housekeeping enzyme that helps to keep us alive.

  • It is produced constitutively i.e. all the time.
  • It protects our stomach, kidney, and platelets etc.
  • They produce prostaglandins (PGE)
    • ​Help the normal function of the stomach wall.
  • It decreases HCl secretion
  • Increases mucus secretion
  • Increases blood perfusion of the stomach wall
    • ​leading to better regeneration.
  • It always protects our stomach from our own HCl.
  • If these are inhibited,
    • gastric ulceration will occur (leading side effect).
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

In case of COX-1 and the kidneys, what does the PGE do?

A
  • PGE dilates the vessels and increases renal blood flow (RBF).
  • If this enzyme is inhibited,
    • vasoconstriction takes place and
    • kidney damage will occur
      • (second most important side effect).
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

In case of the COX-1 which enzyme affects the platelets?

What is its function?

Inhibition of the enzyme leads to?

A
  • Thromboxanes help the aggregation of platelets
    • which leads to normal blood clotting i.e.
  • inhibition of these enzymes leads to bleeding.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Main side effects of COX-1?

A

The three main side effects are:

  1. Gastric ulceration,
  2. kidney damage and
  3. bleeding.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What kind of enzyme is COX-2?

What does it inhibit?

What is it produced by?

A
  • COX-2: This is the primary enzyme in inflammation. This is the inflammatory enzyme. This enzyme inhibits macrophages and fibroblast COX-1 production. It is produced by macrophages and fibroblasts at the site of inflammation and that is why this is the isoenzyme we want to inhibit.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

When we are using NSAIDs, which enzyme are we trying to inhibit?

Give an example of a COX-2 selective NSAID(s)

A
  • Inhibit COX-2 while keeping COX-1 intact i.e.
    • we want drugs that are selectively COX-2 acting.
      • ASPIRIN is NOT COX-2 selective i.e.
        • it can cause gastric ulceration.
  • An example of a COX-2 selective NSAID is
    • MELOXICAM or CARPROFEN.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Where is COX-3 enzyme pressent?

What does it produce and what will it cause?

A

COX-3:

  • A unique enzyme as it is present in the CNS and mainly in the hypothalamus and thalamus of the brain. It will produce prostaglandins, causing fever and enhancing pain sensation.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What happens if you inhibit COX-3?

Which drugs can inhibit COX-3?

A

Inhibiting COX-3

  • Very good antipyretic (reduces fever) effect
  • Analgesic effect
  • NOT causing anti-inflammatory action
    • e.g. PARACETAMOL (METAMIZOLE).
      • These two drugs are not called NSAIDs,
      • but minor analgesics (major being morphine derivatives) as they do not have any anti-inflammatory drug properties.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

COX-2 to COX-1 inhibition rates:

Groups

A

(COX-2 inhibition: COX-1 inhibition)

The higher the ratio, the better the drug.

According to this ratio, we put the drugs into groups.

  1. Older drugs
  2. Second generation = more-selective COX-2 inhibitors
  3. Third generation (the best drugs) = COXIBS.​
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

1st group of drugs = OLDER DRUGS

  1. Drug?
  2. Ratio?
  3. Inhibition?
  4. Safe?
  5. Called?
A
  1. KETOPROFEN and ASPIRIN.
  2. These have a ratio of less than one.
  3. These inhibit both COX-1 and COX-2
  4. Therefore, they are considered UNSAFE
  5. We call these classical NSAIDs.

Ketoprofen, Aspirin

<1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

The second generation of drugs = more-selective COX-2 inhibitors.

  1. Drugs?
  2. Ratio?
  3. Inhibition?
  4. Safety?
A
  1. These include MELOXICAM and CARPROFEN.
  2. These drugs have a ratio of around 10, meaning
  3. They can inhibit COX-2 ten times as much as they inhibit COX-1.
  4. Carprofen (RIMADYL) is lethal in humans?????

Meloxicam

3-10

Carprofen

7-17

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

The third generation (the best drugs)

  1. Called
  2. Drugs
  3. Ratio
  4. Sideeffects
  5. Inhibit
  6. Species specificity
A
  1. COXIBS (best drugs)
  2. DERACOXIB and FIROCOXIB
  3. These usually have extreme ratios.
  4. They cause side effects extremely infrequently because they
  5. ONLY inhibit COX-2.

Deracoxib

22-37

Firocoxib

384

  1. These drugs and their data are for dogs. They have interspecies, interbreed, and interindividual differences.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Pharmacological effects (when it is beneficial)?

A

Pharmacological effects (when it is beneficial):

The most important pharmacological effects are

  1. anti-inflammatory,
  2. analgesic
  3. antipyretic (fever reduction)
  • Platelet aggregation inhibition:
  • Antiendotoxin:
  • Spasmolytic:
  • Antineoplastic:
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Pharmacological effects (when it is beneficial):

  • Platelet aggregation inhibition:
A

Platelet aggregation inhibition:

This is useful in the case of thrombosis where we use ASPIRIN.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Pharmacological effects (when it is beneficial):

Antiendotoxin

  1. Main component and where
  2. Importance
  3. Drugs
  4. Side effects
  5. Bacterial infections
  6. Most frequent drug in horses
A

Antiendotoxin:

  • Endotoxin = main component of the gram-negative bacteria cell wall.
  • In serious gram-negative bacterial infections when bacteria die,
    • endotoxins are released that can kill the patient.
  • FLUNIXIN and MELOXICAM are good antiendotoxins.
  • Endotoxin shock can occur when we are administering antibiotics in gram negative bacterial infection e.g.
    • e coli enteritis,
    • salmonella enteritis,
    • e coli mastitis in cattle
    • colic in horse.
      • This explains why flunixin is the most frequently used drug in horses.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Pharmacological effects (when it is beneficial):

Spasmolytic

  1. Causes
    1. Leading to
  2. Drug
  3. Beneficial in
A

Spasmolytic:

  • It causes smooth muscle inhibition,
    • leading to decreased spasms in the
      • GI tract,
      • urinary tract,
      • genital tract.
  • The drug here is also FLUNIXIN, as well as METAMIZOLE.
  • These spasmolytics are beneficial in
    • colic (any type) and
    • during menstruation (genital spasms).
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Pharmacological effects (when it is beneficial):

Antineoplastic:

  1. When is it caused
  2. What does it produce to require what?
  3. What happens if we inhibit COX?
  4. Drugs used in treatment of Prostate tumors and Urinary bladder tumors
A

Antineoplastic:

  • This is caused because some tumors produce COX enzymes
    • Produce prostaglandins for themselves
      • required for the growth of the tumors i.e.

Inhibit COX = no prostaglandins produced = tumor cannot grow.

  • We use PIROXICAM which has proven useful in the treatment of
    • prostate tumors
    • urinary bladder tumors.
26
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Pharmacokinetics:

Absorption:

  1. NSAIDs are
  2. Forms in the body
  3. Absorbtion through
  4. Production in
  5. Taken with or without food
    1. Types of drugs
A

Absorption:

These are weak acids

They have two forms in the body: ​Ionised form & Non-ionized form.

  • The non-ionized form has good absorption through the membranes
  • Overproduced in the stomach - HCl
  • NSAIDs absorption first in the stomach
    • ASPIRIN = Quick onset

NSAIDS and FOOD

  • Difference in absorption with or without food
  • Week acids = irritable to stomach = WITH FOOD
  • KETOPROFEN, feed decreases its absorption i.e. it is given on an empty stomach.
  • CARPROFEN and MELOXICAM can be given with or without food.
  • MAVACOXIB (canine) has a much better bioavailability when given with food (empty stomach: 20%, full stomach: 80%).
27
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Distribution:

  1. Clinical consequences due to what?
  2. Which clinical consequenses?
  3. Do not combine which drugs?
  4. Why is Loading dose required?
  5. Which drug cannot enter the milk due to the binding of albumin?
A

Distribution:

  • Extensive albumin binding = has some clinical consequences.
    1. The first one is that in hypoalbuminemia,
  • the free drug levels are much higher i.e.
    • toxicity is enhanced.
    • We draw blood and measure the albumin level before administering these drugs.
    • If you give two drugs with high albumin binding, they will compete for the albumin and they can push down the other from albumin leading to increased toxicity i.e.
    • do not combine drugs of high albumin binding.
  • Do not combine NSAIDs or FUROSEMIDE (diuretic) which is also a high albumin binding drug. If this is combined with NSAIDs, you must decrease the dose in order to decrease toxicity.
  1. The other consequence is that loading doses are required i.e.
    * we have to load a higher dose in order to saturate albumin and then we administer a maintenance dose.

MELOXICAM:

Loading dose

Maintenance dose

Dog

  1. 2 mg/kg
  2. 1 mg/kg

Cat (more sensitive)

0.1 mg/kg

as low as 0.02 mg/kg

CARPROFEN:

Loading dose

Maintenance dose

Dog

  1. 4 mg/kg
    1. mg/kg

These cannot enter the milk because they are bound to albumin and only the free form of the drug can penetrate the blood-milk barrier.

Carprofen in cattle has a one-month withdrawal period for meat, and 0 days for milk.

28
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Metabolism:

  1. With?
  2. Which species is this particular acid absent?
  3. Why ?
  4. How to administer knowing this?
  5. Authorized drug for this species?
  6. Long term alternative for this species?
A

Metabolism:

  • Mainly with glucuronic acid,
    • this is absent in cats i.e.
      • the NSAIDs will have a longer half-life in cats as the elimination is slower.
      • This is why we usually administer a smaller dose in cats, or the drugs are given less frequently.
      • There is no drug authorized for cats for more than one week but, we know from studies that
      • MELOXICAM is a good long-term alternative for cats but, again, no drug can officially be licensed for cats.
29
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

A

MANY!!

  1. GI Ulceration
  2. Kidney damage
  3. Hepatotoxicity:
  4. Platelet aggregation inhibition
  5. Methemoglobinemia
  6. Proteoglycan synthesis inhibition
  7. Foetal damage:
  8. Placenta retention:
30
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

GI Ulceration

  1. Where will the ulcerations form
  2. Causes of ulceration
  3. Treatment
  4. How serious is the side effect
A

GI Ulceration:

  • This means that the stomach and duodenum will form ulcers.
  • The two causes of that is firstly,
  1. the local irritation of these weak acids which fall into an ion trap within the cells of the stomach and cause intracellular damage within the cells.
  2. The other reason for gastric damage is that the prostaglandin level will be decreased i.e.
  • Causing GI ulceration even if they are injected. The treatment of this is to use a proton-pump inhibitor (OMEPRAZOLE).
  • This side effect can be life-threatening.
31
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

Kidney damage:

  1. Inhibit what? caused by what?
  2. What does it cause? Leading to?
  3. How many cases of damages takes place?
  4. What is important to remember before you give NSAIDs?
  5. Due to surgery, when can you give NSAIDs?
A

Kidney damage:

  • They inhibit the vasodilation caused by PGE i.e.
    • causes vasoconstriction
    • decrease the perfusion of the kidney
      • leading to kidney damage.

There are 3 cases in which this damage takes place,

  1. When the patient has existing kidney failure i.e.
    1. Examine whether the patient’s kidneys are healthy or not.
  2. In cases of dehydration i.e.
    1. BEFORE you give NSAIDs - hydrate them with perfusion.
  3. During surgery when the patient has been given anesthesia,
    1. kidney perfusion is decreased. because of this i.e.
      1. NSAIDs are only given postoperatively when speaking about surgery.
32
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

  • Hepatotoxicity:
  1. Type of side effect
  2. Frequency of the side effect
  3. Drugs causing hepatotoxicity
A

Hepatotoxicity:

  • Gastric ulceration and kidney damage are outstandingly important side effects with the remaining being additional side effects.
  • HEPATOTOXICITY = Additional side effect
    • This is much less frequent.
  • PARACETAMOL can lead to hepatotoxicity in humans and dogs
    • Metabolized mainly in the liver
      • into NAPQI (N-acetyl-P-benzoquinoneimine) which is its metabolite.
      • This is a very oxidative and reactive metabolite that can damage the hepatic cells.
      • In cats, this NAPQI will oxidize Fe2+ to Fe3+, leading to methemoglobinemia.
  • In CARPROFEN, there are very infrequent idiosyncratic reactions (individual differences), and some individuals are sensitive to this.
    • These are more frequently seen in Labrador or golden retrievers.

In all, hepatotoxicity is much less frequent.

33
Q

PARACETAMOL and HEPATOTOXICITY

  1. Can it lead to hepatotoxicity
  2. In which species
  3. Where is it metabolized
  4. What is its metabolite
  5. Characteristics of the metabolite
  6. What happens to the metabolite in cats?
A

PARACETAMOL can lead to hepatotoxicity

  • in humans and dogs
  • Metabolized mainly in the liver
    • into NAPQI (N-acetyl-P-benzoquinoneimine) which is its metabolite.
    • This is a very oxidative and reactive metabolite that can damage the hepatic cells.
    • In cats, this NAPQI will oxidize Fe2+ to Fe3+, leading to methemoglobinemia.
34
Q

CARPROFEN and HEPATOTOXICITY

A

In CARPROFEN,

  • Very infrequent idiosyncratic reactions
    • (individual differences)
    • Some individuals are sensitive to this.

These are more frequently seen in

  • Labrador
  • Golden retrievers.
35
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

Platelet aggregation inhibition:

  1. When is it beneficial?
  2. When is it non-beneficial and why?
  3. Drugs with potent platelet aggregation inhibition should not be used when?
  4. Types of drugs?
A

Platelet aggregation inhibition:

  • This is beneficial during thrombosis
    • however, it is very non-beneficial during surgery.
  • Drugs that have a potent platelet aggregation inhibitory effect, are not recommended after surgery because after surgery,
    • there can still be bleeding in the wounds/injury site
    1. ASPIRIN
    2. FLUNIXIN
    3. TOLFENAMIC ACID
    4. KETOPROFEN
36
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

  • Methemoglobinemia:
  1. In which species
  2. Caused by what
  3. Color of methemoglobinemia, Color of the blood is?
  4. Which drug can never be given to this species with methemoglobinemia and Why?
A
  1. In CATS,
  2. NAPQI oxidises Fe2+ to Fe3+.
  3. The color of methemoglobinemia is brown i.e.
    • the blood of these cats is chocolate brown.
  4. ​​PARACETAMOL can never be given to cats,
  • it is LETHAL
37
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

Proteoglycan synthesis inhibition

  1. What does it damage?​​
  2. Why is it so bad?
  3. Which drugs causes this damage?
  4. Which drugs are ONLY used in humans?
  5. Which drugs are WITHOUT this damage?
A

Proteoglycan synthesis inhibition = (cartilage damage):

  • Very bad because most of these drugs are
    • Used for patients of arthritis (joint inflammation) and that is why we have to know which ones form cartilage damage
  • ASPIRIN,
  • KETOPROFEN
  • Only used in humans; IBUPROFEN and NAPROXEN
  • MELOXICAM and CARPROFEN
    • have no effect on the cartilage.
38
Q
A
39
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

Foetal damage:

  1. NSAIDs recommended during pregnancy?
  2. In witch part of the pregnancy is the fetus the most sensitive to NSAIDs
  3. Exeption when the pregnant patient has headache - which drug?
A

Foetal damage = TERATOGENICITY

  • These are not recommended during pregnancy,
    • especially during the first trimester.
  • Fetus is most sensitive to drugs in the first trimester.
    • The exception is that if a patient is pregnant and has headaches,
    • METAMAZOLE (minor analgesic, COX inhibitor) has been proven to be safe.
40
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

SIDE EFFECTS

Placenta retention**.

  1. What is Placenta retention?
  2. What does NSAIDs to the which synthesis?
  3. What is Prostaglandins responsible for and why is it so important?
  4. What can take place if this doesn’t happen?
  5. Due to this, when is it not recommended to use NSAIDs to prevent this effect?
  6. What is the only exception?
A

Placenta retention:

  • This is when the placenta stays in the womb.
  • NSAIDs inhibit prostaglandin synthesis.
  • The responsible substance for uterus contraction in order for the placenta to be removed from the womb are prostaglandins i.e.
    • if you remove the synthesis of these prostaglandins =
      • then the uterus cannot contract and placenta retention will take place.
        • Infection and metritis can form from this because it is sensitive to bacterial infections.
  • Because of this, NSAIDs are not recommended 48 hours before and 36 hours after parturition to prevent this side effect.
  • The only exception to this is MELOXICAM.
41
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

A

Acidic substances:

  • These are more irritant to the stomach i.e.
    • more or less causing gastric ulceration more frequently than non-acidic substances
  • All substances contribute to this ulceration.
  1. ​Salicylates:
  2. Propionic acids:
  3. Heteroaryl acetic acids:
  4. Anthranilic acids:
  5. Butyl pyrazolidines:
  6. Oxicams:
42
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Salicylates:

A

Salicylates::

  1. Acetylsalicylic acid:
  2. Na salicylate:
  3. Sulfasalazine, Mesalazine:
43
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Salicylates:

1. Acetylsalicylic acid:

A

Acetylsalicylic acid:

  • ASPIRIN,
    • it is infrequently used in practise, more so for HUMANS.
    • In dogs, it is safe short-term i.e.
      • for a few days.
      • If the owner cannot go to the practice to be administered MELOXICAM, they can be administered aspirin.
    • It is not recommended in cats.
    • In farm animals, mainly in swine and poultry,
      • these are mixed into the water
      • Good painkillers
      • Not that safe.
44
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Salicylates:

2. Na salicylate:

A

Na salicylate:

  • This is much safer
  • More COX-2 selective i.e.
    • Affects the COX-2 enzyme and not the COX-1 enzyme
      • Makes it safer.
  • It is used only in farm animals (poultry, swine, calves)
    • mixed into the water.
45
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Salicylates:

3. Sulfasalazine, Mesalazine:

A

Sulfasalazine, Mesalazine:

  • ONLY used in dogs and humans
    • Treatment of chronic colitis.
  • Crohn’s disease is an painful colitis.
  • These drugs are given orally
  • Large intestine (where the problem is taking place)
    • Release amino-salicylic acid
    • Because drug absorption in the large intestine is of a low level,
      • it will act locally i.e.

These drugs are very safe.

46
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Propionic acids:

A
  1. Ketoprofen:
  2. Vedaprofen:
  3. Carprofen:
47
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Propionic acids:

1. Ketoprofen:

A

Ketoprofen:

  • An older drug,
  • NOT COX-2 selective,
    • significantly inhibiting platelet aggregation i.e.
      • NOT use in bleeding animals or after surgery.
  • ​Interestingly, in cats,
    • it is one of the safest drugs short-term
    • because in cats it has a very short half-life.
    • It is maybe the best anti-pyretic in cats against fever (cats have fever very frequently).
    • Long-term, there can be problems.
48
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Propionic acids:

2. Vedaprofen:

A

Vedaprofen:

  • Exclusively for horses.
  • An oral paste
  • COX-2 selective i.e.
    • Relatively safe.
49
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Propionic acids:

3. Carprofen:

A

Carprofen:

  • It can be given life-long,
  • very safe (COX-2 selective).
  • It can cause liver damage in Labradors and golden retrievers i.e.
    • monitor those liver functions.
  • If given together with other hepatotoxic drugs e.g.
    • PHENOBARBITAL, can be dangerous.
  • In cattle,
    • it has a very long action (4-5 days),
    • leading to a very long withdrawal time (one month) and
    • because of the high albumin binding,
      • milk withdrawal is 0 days.
  • One of the safest drugs we know.
  • It has no cartilage damage
  • Can be used in exotic animals.
50
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

  • Heteroaryl acetic acids:
A

Diclofenac:

  • A very potent and effective in humans for pain and inflammation
  • Highly toxic for:
    • dogs,
    • cats
    • birds
  • Avoid its usage.
51
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Anthranilic acids:

A

Anthranilic acids:

  • 2 drugs
  1. Flinixin
  2. Tolfedine

Flunixin:

  • A platelet aggregation inhibitor i.e.
    • enhances bleeding,
    • anti-endotoxin (colic),
  • Spasmolytic i.e.
    • frequently used in horses.
  • In cattle, the half-life is very short i.e.
    • they produce flunixin-containing pour-on
    • On the back of the animal to provide slower absorption i.e.
    • Onset of action (2-3 days).

Tolfenamic acid (Tolfedine):

  • This also causes bleeding
  • Similarly to ketoprofen = very short half-life in cats i.e.
    • safe short-term drug for cats.
52
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Butyl pyrazolidines:

1. Phenylbutazone:

A

Phenylbutazone:

  • This is used in HORSES and not in other animals.
  • This has two indications in horses,
    • mainly as an ointment (topically) for orthopedic injuries.
53
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Acidic substances:

Oxicams:

A

Oxicams:

  1. Piroxicam:
  2. Meloxicam

Piroxicam

  • A human drug with oncological indications
    • Prostate tumors
    • Urinary bladder tumors.
  • It is NOT used as a painkiller or anti-inflammatory
    • because it is an old classical NSAID = Lots of side effects.

​Meloxicam:

  • It is very safe in all species, humans included.
    • It is also an anti-endotoxin i.e.
      • useful in:
        • enteritis,
        • mastitis and
        • colic.
  • Meloxicam can be injected and given orally.
  • Its dose in dogs is
    • 0.2 mg/kg loading dose
    • 0.1mg/kg maintenance dose.
  • In cats,
    • the loading dose is 0.1 mg/kg.
  • In large animals, the dose is
    • 0.4-0.6 mg/kg.
54
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Non-acidic substances:

A

Non-acidic substances:

  • These have a much more limited effect on the stomach.
  • They are not as ulcerative.
  1. Aniline derivatives
    1. Paracetamol:
  2. Pyrazolines:
    1. Metamizole sodium: ​
55
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Non-acidic substances: ​ Aniline derivatives

A

Non-acidic substances:* *Aniline derivatives

  1. Paracetamol:
  • COX-3 inhibitor,
  • minor analgesic,
  • do NOT give to cats and
  • preferably not in dogs.
  • Be careful that, similarly to carprofen in retrievers,
    • paracetamol in humans has idiosyncratic reactions of hepatic damage.
    • Leading cause of hepatic transplantation in humans.
56
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Non-acidic substances:* ​ *Pyrazolines:

A

Pyrazolines:

  1. Metamizole sodium:
  • Non-specific,
  • COX-3 inhibitor.
  • Mainly acts in the brain
  • Very low activity on COX-1 and COX-2,
    • Very safe
      • no effect on the stomach or kidneys.
  • You can give it to
    • dogs,
    • rodents
  • Cats react with a nervous system of excitation and salivation.
  • Its dose is 20-30 mg/kg.
57
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Coxibs:

A

Coxibs:

  • NB NB NB These are the safest.
  • Absolute COX-2 selectivity.
  • These are the NSAIDs that inhibit COX-2 100 times more than COX-1.

  1. Deracoxib:
  2. Firocoxib:
  3. Robenacoxib:
  4. Cimicoxib:
  5. Mavacoxib
58
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Coxibs

  1. Deracoxib:
A
  1. Deracoxib: Similar to meloxicam but safer, licensed for dogs.
59
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Coxibs

2. Firocoxib:

A

2. Firocoxib: 384:1 i.e. very safe. It is for dogs and horses, orally.

60
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Coxibs

  1. Robenacoxib: and Cimicoxib:
A
  1. Robenacoxib:
  • ​Only coxib licensed for cats
  • Also the only one marketed for injection.
  • For dogs also.
  1. Cimicoxib: Dog tablet.
61
Q

NSAIDS - NON-STEROIDAL ANTI-INFLAMMATORY DRUGS:

Active substances:

Coxibs

Mavacoxib

A
  1. Mavacoxib (NB):
  • Very long half-life in dogs (5-7 days).
  • The duration of action is approx. 3-4 weeks.
  • It is only given to dogs as a tablet.
  • Empty stomach bioavailability is 20%
  • Full stomach bioavailability is 80% i.e.
    • always given with food.
    • It is given orally with food,
    • repeat administration after two weeks and
    • after that, repetition is every four weeks.
  • It is convenient, effective, and safe.

Veterinary Pharmacology (21 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions