Pharmacology Flashcards

(80 cards)

1
Q

pharmacokinetics

A

what a body does to a drug

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2
Q

pharmacodynamics

A

what a drug does to the body

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3
Q

ADME

A

Administration, Distributions, Metabolism, Elimination

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4
Q

Administration

A

Enteral - sublingual, swallowing, rectal
Parenteral - topical, intradermal, subcut, IM, IV, inhalation

IV - accurate control of concentration, used for drugs with narrow safety margins
Inhalation - rapid effect, may cough out, dependent on particle size and tidal volume

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5
Q

Distribution

A

reaches circulation - needs to penetrate tissues

active transport/carrier mediated
passive transport/diffusion
through membrane as pair with ion
can go into fat
must be neutral to cross

cross more rapidly if - neutral, high lipid.water partition in non-ionised compounds, low molecular weight, biological affinity with transporters, small size particles

effect of pH

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6
Q

Metabolism

A

2 phase - catabolic and anabolic - becomes drug derivative and the a water soluble drug
sometimes only 1 phase

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7
Q

Biotransformation

A

non lipid soluble drugs –> oxidised by cytochrome P450 enzymes –> either water soluble product or next phase –> broken down to transferase (water soluble)

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8
Q

liver metabolism

A

broken down by enzymes in the SER of hepatocytes

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9
Q

detoxification

A

forms inactive metabolites - sometimes metabolites produce similar effects to the drug itself

also can break down toxic metabolites

cats & paracetamol - no UTGs so causes methemoglobinuria

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10
Q

Cytochrome P450s (CYP450s)

A

enzymes
mosrtly formed in liver but some in intestinal walls
metabolise drugs
need iron - problem if anaemic

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11
Q

Excretion

A

major routes - renal, biliary, pulmonary
minor routes - mammary, salivary

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12
Q

Drug-drug interactions

A

levels of one drug altered by another
absorption - affected by pH, bacterial flora, decreased gastric emptying
excretion - urine pH and reduced renal excretion
inhibition or induction of enzymes
CYP450s affected by lots of drugs

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13
Q

Therapeutic window

A

concentration where we know there is an effect

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14
Q

TMax

A

maximum effect time

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15
Q

CMax

A

maximum concentration - needs to be below level of toxicity

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16
Q

Rate vs time graphs

A

zero order - flat horizontal line - IV infusion
first order - diagonal up - IM, Subcut, oral - absorption rate proportional to amount of drug

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17
Q

elimination rate

A

amount of drug eliminated per unit time

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18
Q

Initial volume of distribution (Vi)

A

volume of blood + interstitial fluid

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19
Q

Volume of distribution (Vd)

A

volume into which a drug appears to be distributed (litres/kg)

low Vd - mainly accumulated in extracellular fluid
high Vd - drug accumulating in another site (Eg. fat)

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20
Q

total body clearance

A

volume of blood/plasma cleared of parent drug per unit time

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21
Q

bioavailability

A

% of administered dose that reaches the plasma

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22
Q

compartment models

A

one compartment - spreads equally around the body
two compartments - vessel rich groups first then other tissues

vessel rich group –> muscle –> fat

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23
Q

loading dose

A

initial larger dose, followed by constant rate infusion

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24
Q

potency

A

amount of drug needed to produce 50% of maximum effect

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25
efficacy
maximum therapeutic effwct/how well the drug activated receptors
26
affinity
tendency of drug to bind a particular receptor
27
Agonist
produces an effect at a receptor full agonist - 100% activation partial agonist - any less than 100% activation
28
Anatagonist
binds but doesn't produce an effect competitive - competes with agonists at binding sites - curve shifts to right non-competitive - binds to a different site downstream of receptor (ketamine) - curve flattens and moves downward irreversible - dissociates from receptor very slowly or destroys it
29
Inverse agonist
acts on receptor that usually fires on its own to reduce activation
30
therapeutic index
toxic dose/effective dose EC50 - effective concentration - dose needed to reach 50% maximal effect ED50 - effective dose - dose that will produce therapeutic effects in 50% of population
31
receptor types
ion channel cell surface transmembrane receptor ligand regulated enzymes g-protein coupled receptors protein synthesis regulating receptor
32
tachyphylaxis
reduction in tolerance that develops of short period of time - becomes less effective with repeated doses
33
causes of loss of target sensitivity (6)
change in receptors - become resistant to stimulation loss of receptors exhaustion of mediators increased metabolic degradation of drug physiological adaption drug transporters remove drug from target site
34
Opioids
opiates = natural opioids = synthetic mu receptor (kappa in birds) - receptors at point of pain stimulus reduce pain stimulus, reduce signal transmission more receptors at synapse - negative feedback on Ca2+ channels --> hyperpolarisation effect dependent on dose, species, route, stimulus side effects - CVS, pruritus, vomiting
35
Morphine
full agonist - mu, kappa, delta CD2 not licensed in veterinary species (but used anyway)
36
Methadone
full agonist at mu premed, sedation, recovery CD2
37
Meperidine/pethidine
full agonist at mu increased hr (unusual for opiates) CD2 short duration of action
38
Fentanyl
full agonist at mu short acting lipid soluble CRI CD2 bradycardia and slowed respiration following bolus
39
buprenorphine
partial mu agonist long lasting
40
butorphanol
kappa agonist (birds) good sedative, limited analgesia antitussive
41
Local anaesthetics
block sodium channels in nerve fibres becomes active in ionised form (weak bases so ionised at physiological pH) speed of onset related to degree of ionisation potency related to lipid solubility narrow safety margin lidocaine, prilocaine, bupivicaine
42
NSAIDS
COX 1 and COX 2 inhibition - prevents prostaglandin production GIT effects meloxicam, carprofen, aspirin Galliprant - piprant class NSAID - blocks prostaglandins at EP4 rather than COX - should be less side effects contraindications - renal or hepatic failure, hypervolemia, congestive heart failure, pulmonary disease, hemorrhage, slotting problems, spinal injuries, gastric ulceration, steroid use, shock or trauma, pregnancy
43
Alpha-2 Adrenoreceptor Agonist
bind to pre-synaptic alpha 2 receptors - decreased release of neurotransmitters decreased hr and rr synergistic with local anaesthetics medetomidine, dexmedetomidine, xylazine, detomidine, romifidine antagonised by atimpanezole side effects - hypotension followed by hypertension, decrease CO and HR, respiratory depression
44
NMDA antagonists
chronic pain continuously excited NMDA receptor --> continuous pain ketamine
45
local anaesthetic blocks
small animal - splash blocks - epidurals - dental blocks - limb nerve blocks - intraoperative articular blocks horses - diagnostic - epidural - eye and dental - intraoperative and intraarticular farm - cornual - caudal epidural - inverted L - IVRA - paravertebral
46
dental blocks
intraorbital maxillary ophthalmic mental mandibular
47
epidural
spinal column outside dura - post op analgesia, standing surgery or abdominal and hind quarter surgery under GA caudal - between sacral and coccygeal bones - blocks tail and perineum cranial - lumbosacral - all motor sensation to hind limbs complications - accidental vascular injections, hematoma, subarachnoid injection, infection, hypotension, respiratory depression, nerve damage, pruritus, urinary retention, motor dysfunction, hypothermia
48
effects of pain (9)
catecholamine release weight loss wound breakdown hyperglycemia and insulin resistance neutrophilia cytokine production poor immune function reduced appetite post op complications
49
signs of pain (11)
tachycardia tachypnea hypertension/hypotension cardiac arrhythmia pale mm hypersalivation mydriasis sweating trembling increased urination or defacation poor condition
50
pain behaviours
prey species - little pain behaviour abnormal posture, movement, gait, activity reluctance to move agression
51
Glasgow pain scale
canine acute 6 behavioural categories - vocalisation, mobility, response to touch, demeanour, posture, activity score - 0-3/4/5 for each validated
52
cat pain scales
UNESP Botucatu multidimensional Glasgow RCMPS-F
53
Chronic pain scales
none validated for cats or whole body validated osteoarthritis scales for dogs- liverpool osteoarthritis in dogs canine brief pain inventory helsinki chronic pain index canine specific outcome measures
54
Vapours
Nitrous oxide halothane isoflurane sevoflurane desflurane
55
Kinetics of vapour
rate or rise in blood depends on - concentration of agent ventilation cardiac input - inverse solubility of agent in blood - inverse ^ blood:gas coefficient - higher=more soluble
56
Minimum Alveolar Concentration (MAC)
Alveolar concentration producing immobility in 50% of patients in response to a noxious stimulus (for healthy unmedicated patients)
57
MAC affected by:
age nitrous hypotension hypoxia anemia opioids - reduce MAC sedatives - reduce MAC LAs - reduce MAC pregnancy - reduce MAC
58
Vapour MACs
isoflurane = 1.3 haloflurane = 0.9 sevoflurane = 2.2 desflurane = 10.3
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vapour negative effects
CVRS depression formation of reactive species possible negative effects on anaesthetist - bone marrow suppression and foetal abnormalities
60
nitrous oxide
minimal CVRS effects high MAC expensive analgesic greenhouse gas
61
halothane
can cause hepatic necrosis
62
isoflurane
lower solubility - good safer than halothane causes vasodilation - low blood pressure
63
sevoflurane
newer quicker induction than isoflurane less soluble higher MAC but quicker recovery
64
TIVA/PIVA
environmentally friendly additional analgesia reduced MAC of vapour reduced CV depression less pollution and organ toxicity lidocaine - reduces MAC by 25% ketamine - reduces MAC by 30% Alpha-2s Opioids - up to 40% MAC reduction
65
Antibiotics
cell wall synthesis inhibition - penicillin, ampicillin,bacitracin, cephalosporin protein synthesis inhibition - tetracycline, streptomycin cell metabolism inhibition - sulfa drug RNA synthesis inhibition - rifampicin DNA synthesis inhibition - quinolones
66
Antibiotics - adverse effects
toxicity drug interactions reduction in gut flora tissue site necrosis reduced metabolism residues in food producing animals resistance hypersensitivity anaphylaxis
67
Antibiotics - factors influencing success
bacterial susceptability type of tissue local factors - abscess, foreign material, low pH or oxygen wound cleaning and drainage compliance
68
Antibiotic Adjuncts
probiotics anti-tetanus toxin cleaning wounds treat side effects of infection analgesia
69
Antifungals
Polyenes - forms channels in fungal cell membranes Antibiotic - inhibits mitosis Azoles - inhibits ergosterol biosynthesis Allyamines - inhibits ergosterol biosynthesis Thiocarbamates - inhibits ergosterol biosynthesis Antimetabolites - inhibits RNA and DNA synthesis Profens - direct damage to fungal cytoplasmic membranes
70
Ringworm (dermatophytosis)
ring shaped lesions zoonotic fungal spores long lived in the environment prevention - cleaning and disinfection, carrier control (cats) treatment - hair clipping, ketnoazole (dog), itraconazole (cat), topical treatment, treat animals in contact, biosecurity self limiting but can last 4-9 months - danger to immunocomprised people
71
Aspergillosis
commensal in most domestic animals different forms - pulmonary, mycotic abortion, guttural pouch mycosis, nasal and paranasal, asymptomatic diagnosis - radiograph (turbinate destruction), rhinoscopy (fungal plaques), can't just culture - commensal treatment - topical clotrimazole (needs to stay in place on fungal plaques for an hour - anaesthetic), surgical exposure and curettage, topical potassium iodide applied with endoscope
72
viral replication stages (5)
cell entry uncoating control of host protein and nucleic acid synthesis to make viral components assembly release
73
Antivirals
narrow therapeutic margin target viral function or cellular function that virus needs only a few and not effective against many pathogens potential for resistance in human pathogens some virostatic - need adequate host immune response virbagen omega - only one licensed in animals - FIV, feline leukemia and parvo - doesn't go into cell, releases interferon to increase cell resistance some used unlicensed
74
feline infectious peritonitis
feline coronavirus usually asymptomatic diarrhea in kittens wet form - fluid accululation in abdomen dry - inappetance, jaundice, diarrheoa, weight loss, ocular or neurological signs raised bilirubin without raised liver enzymes
75
vaccine types
inactivated - more expensive, needs adjuvant, more stable, no chance of reversion attenuated - cheaper, no adjuvant needed, less stable, can revert MRNA - quick to produce, more expensive, can't revert
76
horse vaccines
equine flu tetanus equine herpes equine rotavirus strangles recorded in horse passport
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cattle
BVD Infectious bovine rhinotracheitis calf enteric disease pneumonia mastitis salmonella bluetongue
78
dogs
core - distemper - parvo - adenovirus/infectious canine hepatitis - lepto non-core - kennel cough - rabies - leishmaniases - canine herpes virus
79
cats
core - enteritis - calicivirus - feline herpes virus non-core - FeLV - chlamydia - rabies - bortadella bronchisepta
80
rabbits
myxo rabbit viral haemorrhagic disease