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Pharmacology > Misc: Local Anaesthetics, antihistamines, immunosuppresants > Flashcards

Misc: Local Anaesthetics, antihistamines, immunosuppresants Flashcards

1
Q

What is the mechanism of action of local anaesthetics?

A

Block sodium channels

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2
Q

Why would hyaluronidase be used with a local anaesthetic?

A

Improved diffusion through SQ tissue

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3
Q

What are the toxic effects of systemic absorption of local anaesthetics?

A

Excitability followed by depression of CNS

Depression of cardiovascular system

Vasodilation and hypotension

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4
Q

List five local anaesthetics

A

Procaine

Lignocaine

Buvipicaine

Mepivicaine

Benzocaine

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5
Q

List two local anaesthetics used used in topical opthalmology preparations

A

Proparacaine

Tetracaine

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6
Q

Which cells store histamine?

A

Mast cells, basophils, platelets

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7
Q

Where are histamine levels normally highest?

A

GIT, lungs, skin

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8
Q

What is the result of activating histamine receptor H1?

A

Arteriole dilation

Contraction of GIT and bronchiolar smooth muscle

Constriction of large arteries and veins

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9
Q

What is the result of activating histamine receptor H2?

A

Arteriolar dilation

Increased gastric acid secretion

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10
Q

What is the result of activating histamine receptor H3?

A

CNS neurotransmitter mediator

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11
Q

What is the result of activating histamine receptor H4?

A

Unknown, but possible role in asthma

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12
Q

What are the overall results of activating histamine receptors (H1-H4)?

A

Constriction of large vessels, GIT, bronchi

Relaxation of arterioles (hypotension)

Increased capillary permeability

Increased gastric acid secretion

Sensitization of nociceptors

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13
Q

What is the mechanism of action of antihistamines?

A

H1 or H2 antagonists

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14
Q

What is a consideration of using antihistamines in ruminants?

A

Not orally active in ruminants

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15
Q

What are some indications for use of H1 antagonists?

A

Management of allergic pruriritis in dogs/cats

Management of systemic anaphylaxis (following emergency treatment)

Motion sickness

Mild sedatives (drowsiness)

Asthma or chronic airway hyperresponsiveness

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16
Q

What are the indications for H2 antagonists?

A

Reduce gastric acid production

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17
Q

What are the main side effects of antihistamines?

A

CNS depression (common)

Excitement

GIT disturbance

Anticholinergic effects (dry mouth, urinary retention)

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18
Q

List four antihistamines that cross the BBB

A

Diphenhydramine (Benadryl)

Promethazine

Chlorpheramine

Amitryptiline (tricyclic)

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19
Q

List two antihistamines that do not cross the BBB

A

Loratadine (Claratyne)

Ceterizine (Zyrtec)

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20
Q

What is the difference between an anaphylactic and anaphylactoid reaction?

A

Anaphylactic: Type 1 hypersensitivity; requires previous exposure

Anaphylactoid: occurs without previous exposure, not mediated by IgE

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21
Q

What is the outcome of an anaphylactic/anaphylactoid reaction?

A

Severe hypotension

Reduced cardiac output

Airway restriction

Laryngeal oedema

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22
Q

What is the treatment for anaphylaxis?

A

Adrenaline (Epipen)

Stabilises membranes, stops hypotension

Increased CO, BP, bronchodilation; antiinflammatory and anthistamine

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23
Q

List five immunosuppressive drugs

A

Glucocorticosteroids

Cyclosporine

Tacrolimus

Cyclophosphamide

Thiopurines

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24
Q

What are the indications for cyclosporine?

A

Immune mediated disease (atopic dermatitis, IHMA, IBD)

Preventing transplant rejection

25
Q

What is the mechanism of action of cyclosporine?

A

Blocks calcineurin > Inhibits T cell function & cytokine release

26
Q

What are some considerations of administering cyclosporin?

A

Poorly absored PO

Various formulations not bioequivalent

27
Q

What are the adverse effects of cyclosporine?

A

vomiting

diarrhoea

anorexia

28
Q

What is the mechanism of action of tacrolimus?

A

Macrolide: Inhibits calcineurin > Inhibits T cell activity

29
Q

What are the indications for tacrolimus?

A

Immune mediated diseases (atopic dermatitis, IMHA, IBD)

Prevent transplant rejection

30
Q

What are the considerations for administration of Tacrolimus?

A

Poor oral absorption & possibly toxic

Useful topically

31
Q

What is the mechanism of action of oclacitinib?

A

Inhibits cytokines, especially IL-31 (associated with pruritis)

32
Q

What are the side effects of oclacitinib?

A

Minor

33
Q

What is the mechanism of action of cytopoint?

A

Monoclonal antibody therapy: Inhibits IL-31

34
Q

What is the mechanism of action of cyclophosphamide?

A

Alkylates (damages) DNA of B and T cells

35
Q

What are the indications of cyclophosphamide?

A

Antineoplastic and immunosuppressive

SLE (systemic lupus erythamatosus), IMHA, RA (rhumatoid arthritis)

36
Q

What are the side effects of Cyclophosphamide?

A

myelosuppression

vomiting

diarrhoea

alopecia

sterile haemorrhagic cystitis and bone marrow suppression

37
Q

Name three thiopurines

A

6-thioguanidine (6-TG)

Mercaptopurine (6-MP)

Azathioprine

38
Q

What is the mechanism of action of thiopurines?

A

Purine antimetabolites: Inhibit purine synthesis (DNA/RNA) > inhibits synthesis of WBC > Immunosuppression

39
Q

What are the indications of 6-TG and 6-MP

A

Mainly antineoplastic

40
Q

What are the indications of azathioprine?

A

Immunosuppressive (IMHA, HA, IBD, adjunct for myaestheia gravis)

41
Q

What are the two main categories of dermal pharmacology?

A

Transdermal

Topical

42
Q

What are the functions of skin?

A

Sensory perception (touch, pressure, itch, pain, temperature)

Protection (physical, microbes, solar radiation, water loss)

Secretion (sweat, sebum)

Vit D production

Immune and temperature regulation

43
Q

What are some of the outcomes of imbalance in the skin caused by disease/trauma?

A

Nociception

Proliferation of keratinocytes

Epidermal hyperplasia

Ulceration

Pruritis

44
Q

What factors are important to consider when using dermal penetration of a drug (transdermal administration)?

A

Drug type (Vehicle, molecular weight, lipid/water soluability)

Skin condition: intact keratinocyte layer difficult to penetrate, especially when dry

Cutaneous blood flow (can be affected by temperature)

45
Q

What are important considerations when designing transdermal drugs?

A
  • lipid soluability in passing through stratum corneum
  • water soluability in lower layers
  • vehicle must be able to release drugs
  • many agents metabolised by skin: poor systemic availability
  • some agents (e.g. fipronil) remain localised
  • membrane of patches control rate of drug release
46
Q

List two examples of transdermal drugs

A

Fentanyl

Macrocyclic lactones

47
Q

What four factors important in the success of topical pharmacology?

A

The disease/condition

The patient

The owner

The environment

48
Q

What disease factors are important in topical pharmacology?

A

Sebhorrhic disorders usually secondary to infection, allergy, or hormone disorder

Pruritic disorders: often benefit from antipruritic agents

49
Q

What patient factors are important in success of topical pharmacology?

A

Species, size, haircoat, temperment

50
Q

What owner factors are important in the success of topical pharmacology?

A

Time, level of dedication, cost, ability

51
Q

What environmental factors are important in the success of topical pharmacology?

A

Season, allergen, other pets

52
Q

List three antiseborrhic agents

A

Sulfur

Salicylic acid

Tar

(e.g. anti-dandruff shampoos that soften cells and rehydrate skin)

53
Q

List three groups of antipruritic topical agents

A

Emmolients

Moisturising agents

Glucocorticoids/antihistamines

54
Q

List two topical emmolient antipruritic agents

A

Lanolin, olive oil

55
Q

How do emmolients work as antipruritic agents?

A

Form an occlusive layer and prevent water loss

56
Q

List a topical moisturising antipruritic agent

A

Glycerin

57
Q

How does glycerin work as a topical antipruritic agent?

A

Increase fatty acid concentration and prevent water loss

58
Q

List four topical antimicrobial agents

A

Benzoyl peroxide

Chlorhexidine

Iodine

Miconazole

59
Q

What drug classes might be included in a formulation for otitis?

A

Antibacterials

Antifungals

Antiparasitics

Anti-inflammatories

Anaesthetic

Pharmacology (12 decks)

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