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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
What is the mechanism of action of cyclosporine?
Blocks calcineurin \> Inhibits T cell function & cytokine release
26
What are some considerations of administering cyclosporin?
Poorly absored PO Various formulations not bioequivalent
27
What are the adverse effects of cyclosporine?
vomiting diarrhoea anorexia
28
What is the mechanism of action of tacrolimus?
Macrolide: Inhibits calcineurin \> Inhibits T cell activity
29
What are the indications for tacrolimus?
Immune mediated diseases (atopic dermatitis, IMHA, IBD) Prevent transplant rejection
30
What are the considerations for administration of Tacrolimus?
Poor oral absorption & possibly toxic Useful topically
31
What is the mechanism of action of oclacitinib?
Inhibits cytokines, especially IL-31 (associated with pruritis)
32
What are the side effects of oclacitinib?
Minor
33
What is the mechanism of action of cytopoint?
Monoclonal antibody therapy: Inhibits IL-31
34
What is the mechanism of action of cyclophosphamide?
Alkylates (damages) DNA of B and T cells
35
What are the indications of cyclophosphamide?
Antineoplastic and immunosuppressive SLE (systemic lupus erythamatosus), IMHA, RA (rhumatoid arthritis)
36
What are the side effects of Cyclophosphamide?
myelosuppression vomiting diarrhoea alopecia sterile haemorrhagic cystitis and bone marrow suppression
37
Name three thiopurines
6-thioguanidine (6-TG) Mercaptopurine (6-MP) Azathioprine
38
What is the mechanism of action of thiopurines?
Purine antimetabolites: Inhibit purine synthesis (DNA/RNA) \> inhibits synthesis of WBC \> Immunosuppression
39
What are the indications of 6-TG and 6-MP
Mainly antineoplastic
40
What are the indications of azathioprine?
Immunosuppressive (IMHA, HA, IBD, adjunct for myaestheia gravis)
41
What are the two main categories of dermal pharmacology?
Transdermal Topical
42
What are the functions of skin?
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
What are some of the outcomes of imbalance in the skin caused by disease/trauma?
Nociception Proliferation of keratinocytes Epidermal hyperplasia Ulceration Pruritis
44
What factors are important to consider when using dermal penetration of a drug (transdermal administration)?
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
What are important considerations when designing transdermal drugs?
- 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
List two examples of transdermal drugs
Fentanyl Macrocyclic lactones
47
What four factors important in the success of topical pharmacology?
The disease/condition The patient The owner The environment
48
What disease factors are important in topical pharmacology?
Sebhorrhic disorders usually secondary to infection, allergy, or hormone disorder Pruritic disorders: often benefit from antipruritic agents
49
What patient factors are important in success of topical pharmacology?
Species, size, haircoat, temperment
50
What owner factors are important in the success of topical pharmacology?
Time, level of dedication, cost, ability
51
What environmental factors are important in the success of topical pharmacology?
Season, allergen, other pets
52
List three antiseborrhic agents
Sulfur Salicylic acid Tar (e.g. anti-dandruff shampoos that soften cells and rehydrate skin)
53
List three groups of antipruritic topical agents
Emmolients Moisturising agents Glucocorticoids/antihistamines
54
List two topical emmolient antipruritic agents
Lanolin, olive oil
55
How do emmolients work as antipruritic agents?
Form an occlusive layer and prevent water loss
56
List a topical moisturising antipruritic agent
Glycerin
57
How does glycerin work as a topical antipruritic agent?
Increase fatty acid concentration and prevent water loss
58
List four topical antimicrobial agents
Benzoyl peroxide Chlorhexidine Iodine Miconazole
59
What drug classes might be included in a formulation for otitis?
Antibacterials Antifungals Antiparasitics Anti-inflammatories Anaesthetic

Pharmacology (12 decks)

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