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Pharmacology > Antiinflammatory and Immunosuppressive drugs > Flashcards

Antiinflammatory and Immunosuppressive drugs Flashcards

1
Q

Physiological properties of Glucocorticoids

A

Diabetogenic

Gluconeogenesis increases –> Hyperglycaemia

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2
Q

Pathological properties of Glucocorticoids

A

Muscle atrophy (weakness)
Osteoporosis (decreased calcium absorption)
Delayed wound healing (decreased collagen synthesis)
Skin thinning, alopecia
Decreased growth
Polyuria/polydipsia (ADG inhibition and psychic)

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3
Q

Pharmacological properties of Glucocorticoids

A 
Antiinflammatory
Antiallergic
Immunosuppressive
Antishock
Neuroprotective
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4
Q

What does Glucocorticoids inhibit?

A

It inhibits the production of Phospholipase A2 (PLA2), therefore inhibiting the production of LOX, COX1,2&3, and EOX

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5
Q

Antiinflammatory and Immunosuppressive effects of GC

A

Decreased COX enzyme expression
Decreased interleukin expression (especially IL1 & 2)
Decreased synthesis of TNF and IFN synthesis
Apoptosis in lymphocytes (lymphocytopenia)
Neutrophilia

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6
Q

Antishock effect of GC

A

Decreased capillary membrane permeability –> enhances microcirculation
In high dosage: vasoconstriction

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7
Q

Neuroprotective effect of GC

A

Local vasoconstriction

Counteract lipidperoxidation and enhances microcirculation

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8
Q

Cortisol

A

GC
Relative potency: 1
Effect: Short

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9
Q

Prednisolone

A

GC
Relative potency: 4
Dosage: 0,5-1 mg/kg 24h
Effect: Medium

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10
Q

Methylprednisolone

A

GC
Relative potency: 5-7
Effect: Medium

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11
Q

Triamcinolone

A

GC
Relative potency: 5-10
Effect: Medium

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12
Q

Betamethasone

A

GC
Relative effect: 25-30
Effect: Long

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13
Q

Dexamethasone

A

GC
Relative effect: 25-30
Effect: Long

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14
Q

Beclomethason

A

GC
Relative potency: 300-400
Effect: Local

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15
Q

Fluticason

A

GC
Relative potency: 400-500
Effect: Local

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16
Q

Budesonide

A

GC

Effect: Oral

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17
Q

Active substances GC (9)

A 
Cortisol
Prednisolone
Methylprednisolone
Triamcinolone
Betamethasone
Dexamethasone
Beclomethason
Fluticason
Budesonide
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18
Q

Side effects of GC (11)

A
  1. Hypothalamus-hypophysis-adrenal cortex axis inhibition (atrophy, addison’s disease)
  2. Gastric ulcers
  3. Hepatopathy (ALKP increases)
  4. Pancreatitis
  5. Glaucoma. cataracta
  6. Thinning of skin, delayed wound healing, alopecia
  7. Polyuria/Polydipsia
  8. Polyphagia
  9. Remobilizing fats (stomach or face)
  10. Muscle atrophy
  11. Immunosupression
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19
Q

Systemic use of GC

A
  1. High dosage once
  2. Alternate day therapy (prednisolone and Methylprednisolone)
  3. Long acting injections
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20
Q

Indication of GC

A
  1. Local usage (atopic dermatitis, otitis externa, mastitis)
  2. Single injectable dose
  3. Asthma, RAO –> inhalation usage
  4. Intraarticular
  5. ADT
  6. Depot injection
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21
Q

What does NSAIDs inhibit?

A

NSAIDs inhibit the production of COX (PGF, PGE, PGI, TX, prostaglandins and Thromboxins)

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22
Q

Mechanism of COX-1

A

Located in the stomach, kidney and platelets, present all the time to protect us
Kidney: Dilate vessels, increase renal blood flow
Platelets: Aid in coagulation
Stomach: Increase mucous production, decrease acid production and increase regeneration rate.

Inhibition therefore leads to vasoconstriction, no coagulation and gastric ulcers

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23
Q

Mechanism of COX-2

A

Macrophages and fibroblasts.

It is inductive, so it is only present during inflammation.

24
Q

Mechanism of COX-3

A

Sensation of pain and fever. So it is not a NSAID persay but more a minor analgesic.

25
Q

COX2:COX1 ratio

A 
Ketoprofen, aspirin: <1 (not safe)
Meloxicam: 3-10
Carprofen: 7-17
Deracoxib: 22-37
Firocoxib: 384 (very safe!)
26
Q

Pharmacological effects of NSAIDs

A

Antiinflammatory
Analgesic
Antipyretic

\+
Platelet aggregation inhibition
Antiendotoxin
Spasmolytic
Antineoplastic
27
Q

Side effects of NSAIDs (10)

A
  1. GI ulceration (local irritation (ion trapping) and decreased PGE)
  2. Kidney damage
  3. Hepatotoxicity (Paracetamol, carprofen)
  4. Platelet aggregation inhibition
  5. Allergic reaction
  6. Methaemoglobinaemia (Paracetamol in cat)
  7. Proteoglycan synthesis inhibition (cartilage damage) (aspirin, ketoprofen, ibuprofen, naproxen)
  8. Fetal damage
  9. Placenta retention
  10. Cardiotoxicity
28
Q

Acidic substances (NSAIDs)

A 
Salicylates
Arilpropionic acid
Heteroaryl acetic acids
Anthranilic acids
Butyl pyrazolidines
Oxicams
29
Q

Salicylates

A

NSAIDs
Aspirin (Acetylsalycilic acid)
Na-salicylate
Sulfasalazine, mesalazine

30
Q

Arilpropionic acids

A

NSAIDs
Ketoprofen
Vedaprofen
Carprofen

31
Q

Carprofen

A

NSAIDs
PO, SC, IV dose: 4.4–> 2.2 mg/kg)
COX-2 preferential, no cartilage damage, rarely side effects.
Ibuprofen, naproxen: DON’T

32
Q

Heteroaryl acetic acids

A

NSAIDs

Etodolac

33
Q

Anthranilic acids

A

NSAIDs
Flunixin meglumine
Tolfenamic acid (safe short term also in cats)

34
Q

Butyl pyrazolidines

A

NSAIDs

Phenylbutazone

35
Q

Oxicams

A

NSAIDs
Piroxicam
Meloxicam

36
Q

Meloxicam

A

NSAIDs
COX-2 preferential
0.2–> 0.1 mg/kg SID in dogs and cats
0.4-0.6 mg/kg in large animals

37
Q

Non acidic substances (NSAIDs)

A

Anilin derivatives

Pyrazolones

38
Q

Anilin derivatives

A

NSAIDs

Paracetamol (COX-3 inhibition!), NEVER IN CATS!! (Methaemoglobinaemia)

39
Q

Pyrazolones

A

NSAIDs
Metamizole sodium
Mainly COX3

40
Q

Coxibs

A

NSAIDs
Deracoxib (dog)
Firocoxib (highly COX2 selective) (Dog and horse)
Robenacoxib (dog/cat)
Cimicoxib
Mavacoxib (long half life, dog, 98% albumin binding)

41
Q

JAK inhibitors indications

A

Rheumatoid arthritis
Crohn disease
Leukemias
Alopecia

42
Q

JAK inhibitor in veterinary use

A

Oclacitinib for atopic dermatitis. inhibits IL-4, IL-13 and IL31. + CYP450 is not involved

43
Q

Pharmacological effects of JAK inhibitors

A

Antiinflammatory
Antiallergic
Antipruritus

44
Q

Side effects of JAK inhibitors

A 
UTI
Vomiting
Otitis
Pyoderma
Diarrhoea
45
Q

Lokivetmab

A

Target Canine interleukin 31, against itching.

46
Q

Antihistamines indications

A 
Against anaphylactic shock
Atopic dermatitis
Flea allergy dermatitis
Premedication
Asthma, RAO
47
Q

Mechanism of action (Antihistamines)

A

Inverse agonists

48
Q

1st generation (antihistamines)

A

Sedation is more frequent. they are non-ionized and can cross the BBB, leading to sedation, they also have a low albumin binding.
Ethylenediamines: Chloropyramin, chlorpheniramine
Ethanolamines: Diphenhydramine, dimenhydrinate (highly recommended to give before vaccine is given)
Phenothiaxines: promethazine
Piperazines: hydroxyzine (best for atopic dermatitis)
Others: dimetinden, cyproheptadine (has a appetite stimulant as well)
CYP450 interaction!!

49
Q

2nd generation (antihistamines)

A

Ionized and high albumin binding, so the BBB is not crossed. Preferred in human medicine.
Ioratadine, cetrizine, levocetirizine

50
Q

Side effects (antihistamines)

A 
CNS depression (1st gen)
Cardiac toxicity (1st gen in humans)
Anticholinergic effect (1st gen)
Appetite depression (except cyproheptadine)
51
Q

Immunosupression indications

A 
Autoimmune diseases (Lupus, IHA, KCS)
Hypersensitivity diseases (Atopic dermatitis, asthma, IBD)
Transplantation
52
Q

Immunosupressive drugs

A

Antimetabolites
Alkylating agents
GLucocorticoids
Cytokine gene expression inhibitors

53
Q

Antimetabolites

A

Immunesupressive drugs
Purine-analogues (Azathioprin, mycophenolate-mofetil)
Pyrimidine-analogues (Leflucomide)
Folic acid antagonists (Methotrexate –> Apoptosis of activated T-cells)

54
Q

Alkylating agents

A

Immunesupressive drugs

Cyclophosphamide (B & T-cell equally affected) (GI and BM side effects)

55
Q

Cytokine gene expression inhibitors

A

Immunesupressive drugs

Calcineurin-inhibitors (cyclosporine, tacrolimus, pimecrolimus)

56
Q

Purine and pyrimidine analogues

A

Immunosupressive drugs
Inhibition or DNA damage. effect on the cell division
Azathioprin (prodrug –> slow release, longer effect, can be given IV or PO)
Mycophenolate-mofetil (Prodrug –> PO, especially specific to T and B-lymphocytes, much safer, rarely used in veterinary medicine)

57
Q

Cyclosporin

A

Immunosupressive drug
Mastocyte inhibition, decreased IL and TNF expression
PO 5 mg/kg in dog, 7 mg/kg Fe and locally
Side effects: vomiting, diarrhoea, alopecia, gingival hyperplasia

Pharmacology (7 decks)

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