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Therapeutics Flashcards

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1
Q

Commonly used pain relief in equine practice

A

NSAIDs

Opioids

Paracetamol

Hospital based: ketamine and lidocaine

Others: Gabapentin, pregabalin, local anaesthetics

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2
Q

Primary mode of action of NSAIDs

A

Inhibition of COX enzymes, thereby limiting prstaglandin synthesis

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3
Q

Common NSAIDs used in equine practice

A

Phenylbutazone

Suxibuzone

Flunixin

Meloxicam

Firocoxib

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4
Q

Trade name of phenylbutazone

A

Equipalazone

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5
Q

Trade name of suxibuzone

A

Danilon

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6
Q

Trade names of flunixin in horses

A

Cronyxin
Allenyxin

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7
Q

Trade names of meloxicam for horses

A

Rheumocam
Meloxicam

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8
Q

Trade name of firocoxib in horses

A

Equioxx

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9
Q

Routes of administration available for phenylbutazone

A

Oral - granules

IV - liquid

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10
Q

Routes of administration of suxbuzone (danilon)

A

PO - micro encapsulated granules so might be more palatable that phenylbutazone

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11
Q

Routes of administration of flunixin

A

PO - paste

IV (??)

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12
Q

Routes of administration of meloxicam in horses

A

PO- liquid (banana flavour)

IV - liquid

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13
Q

Routes of administration of firocoxib (equioxx)

A

PO - tablet

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14
Q

Which NSAIDs must horses be signed out of the food chain for?

A

Phenylbutazone or suxibuzone

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15
Q

Which drugs must not be used in horses classified as food producing animals?

A

Phenylbutazone

Pergolide (prascend)

Metronidazole

Chloramphenicol

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16
Q

Where are NSAIDs metabolised

A

Liver - so be careful with heatopathy cases

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17
Q

NSAID induced colitis in horses

A

Right dorsal colitis - protein losing enteropathies

Can present as low grade colic or symptoms of PLE, such as hypoalbuminaemia on biochemistry or dependent oedema

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18
Q

How do opioids work?

A

Opioid receptors distributed throughout the CNS and within peripheral tissue

μ receptors agonists indirectly stimulate descending inhibitory pathways to activate descending inhibitory neurons.

Increased inhibition = reduction of nociceptive transmission from the periphery to the thalamus.

Exogenous and endogenous opioids can also exert a direct inhibitory effect upon the substantia gelatinosa (in the dorsal horn) and peripheral nociceptive afferent neurones, reducing nociceptive transmission from the periphery.

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19
Q

Commonly used opioids in horses

A

Morphine

Methadone

Butorphanol

Buprenorphine

Fentanyl

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20
Q

Morphine and methadone

A

μ-agonist opioids

IM or IV (under sedation)

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21
Q

Butorphanol

A

μ-antagonist opioids, κ-agonist

IV

Rarely considered analgesic, used in combination with an alpha-2 for sedation

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22
Q

Buprenorphine

A

partial μ-agonist opioids

IV

Rarely used as expensive and anecdotally less efficacious

Longer acting than morphine, but longer ileus effects as well

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23
Q

Fentanyl

A

Transcutaneous patches, most commonly seen in foals, short acting unless transdermal

Relatively short acting potent μ-agonist opioid

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24
Q

What do we need to be aware of when using opioids?

A

Locomotor stimulation

Ileus

Controlled drugs: methadone, fentanyl, morphine (pethidine): Schedule II Dangerous Drugs (see Appendix)

Respiratory depression

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25
How does paracetamol work?
A weak inhibitor of the synthesis of prostaglandins (PGs) However, the in vivo effects of paracetamol are similar to those of the selective cyclooxygenase-2 (COX-2) inhibitors Poor anti-inflammatory
26
How is paracetamol used in horses?
Generally given orally, under cascade closest formulation in pracetam for pigs Avoid in cases of hepatopathy
27
Lidocaine MoA
Desensitise nerves: sodium channel blockers which prevent propagation of depolarising action potentials by the nodes of Ranvier.
28
Which three local anaesthetics can be used in horses?
Lidocaine Mepicaine Bupivacaine
29
Why might lidocaine be used after colic surgery?
Lidocaine is arguably a prokinetic and is believed to enhance the return of intestinal activity after colic surgery.
30
Ketamine MoA
NMDA antagonist, but its mechanisms are complex and still being investigated Analgesic, or rather anti-nociceptive, effects are thought to be associated with ketamine’s augmentation of delta opioid receptors, alongside aminergic (anti-nociceptive) pathways.
31
Lidocaine CRI
Intra-operatively to reduce volatile agent requirements and provide analgesia, or post-surgically for analgesia and potentially as a prokinetic, although prokinetic activity may be solely derived from reducing pain
32
Use of ketamine in horses
IV, IV CRI, IM TIVA GA induction Epidural
33
What do we need to be aware of before using ketamine?
schedule 2 controlled drug Horses must be assessed for dysphoria; profound psychotomimesis and hypnosis in humans
34
What do we need to be aware of before we use lidocaine?
extra-pyramidal effects; Lidocaine overdose leads to CNS effects, including muscle tremors and ataxia, and a potential for cardiac dysrhythmias, therefore careful monitoring is required.
35
Commonly used antibiotics in horses
Trimethoprim sulphadiazine (TMPS) Penicillin Gentamycin Metronidazole Oxytetracycline Doxycycline Enrofloxacin Ceftiofur (protected) Amikacin (foals IV, adults within joint/IVRP)
36
How does TMPS work?
Sulphonamides: prevent incorporation of PABA into folic acid in bacterial cells (bacteriostatic) Trimethoprim: inhibits folate synthesis – acts synergistically to be bacteriocidal Time-dependent killing Lipid soluble; good distribution around the body Hepatic metabolism, renal excretion
37
What spectrum is TMPS?
Theoretically broad spectrum but not good for anaerobes
38
Uses of TMPS
UTD, LRT, UTI, placentitis, epididymitis, renal concentration Theoretically meningitis and peritonitis Widespread resistance
39
Which pathogens show most resistance to TMPS?
Pseudomonas, klebsiella, mycoplasma
40
When is TMS not useful?
Necrotic tissue or pus
41
Possible adverse effects of TMPS
Neutropaenia Colitis, diarrhoea (dysbiosis of gut microbiota) Never use with concurrent alpha-2 - dysrhythmia, hypotension, death
42
How does penicillin work?
inhibition of cell wall synthesis; PBPs (penicillin binding proteins) and transpeptidase prevent incorporation of peptidoglycans into cells walls leading to cell lysis hence effective action against G+ bacteria and anaerobes
43
Spectrum of penicillin
Effective against G+ bacteria and anaerobes. Some limited G-ve activity but not to be considered broad-spectrum (Pasteurella, Actinobacillus).
44
Resistance to penicillins
Some resistant staphs, alpha-strep, and Rhodococcus Bacteroides fragillis
45
How do aminoglycosides work?
Act synergistically to provide broad-spectrum cover. Inhibition of polypeptide synthesis creates aerobic, g-ve activity. It does this by being pumped across cell membranes and binding 30S ribosomes. Poor tissue penetration; work best in alkaline environments – poor action in acidic/necrotic tissue Uptake is decreased in low-oxygen environments Concentration-dependent killing
46
Use of procaine penicillin
IM, never IV Rotate injection sites
47
Use of crystapen
Not complexed with procaine so can be used IV Pre-operative, rapid action
48
Use of gentamycin
Can cause myositis if IM Intra-articular and IVRP use for joint infections - thought to be low chondrotoxicity
49
What happens if you use procaine penicillin IV?
Seizure, death
50
Possible adverse effects to penicillin
Resistance Myositis and focal pain (IM injections) Allergy Haemolytic anaemia Antimicrobial associated colitis
51
Possible adverse effects of aminoglycosides
Nephrotoxicity Ototoxicity Neuromuscular blockade
52
How does metronidazole work?
Bacteriocidal - extensively damages DNA and inhibits DNA repair Concentration dependant killing Narrow spectrum - anaerobes and many protozoa Wide distribution, good penetration Hepatic metabolism, renal excretion
53
Common uses for metronidazole
Anaerobes Generally used in polypharmacy Bone penetration, peritonitis, synovial fluid, abscesses, CNS Oral, rectal, topical
54
What do you need to be aware of before using metronidazole?
Colitis Neurological signs Anorexia – bad taste if given orally Some side effects reported in lab animals (carcinogenic) or humans (teratogenic in 1st trimester)
55
How do tetracyclines work?
Bacteriostatic but bacteriocidal at higher concentrations Inhibits bacterial protein synthesis - reversible binding of the 30S ribosomal subunit Concentration dependent killing
56
Spectrum of tetracyclines
Broad spectrum for aerobes. Particularly efficacious for infections caused by Ehrlichia, Anaplasma and Rickettsia sp. Variable against anaerobes, main resistance from Bacteroides and Clostridia Not effective against Proteus and Pseudomonas Variable efficacy against Enterococci, Streptococcus and Staphylococcus
57
Distribution of tetracyclines
Well distributed except in the CNS
58
59
Metabolism of tetracyclines
Significant enterohepatic recycling and eliminated in urine (doxycycline orally is eliminated in faeces)
60
Commonly used forms of tetracyclines
Oral: doxycycline - variable absorption IV: oxytetracycline
61
What are tetracyclines commonly used for in horses?
Lyme disease, leptospirosis, Lawsonia (foals), lower respiratory disease (foals)
62
What do we need to be aware of before we use tetracyclines?
Renal tubular necrosis (oxy>doxy) Hypotension and collapse with rapid IV oxytetracycline Fatal cadiovascular events if doxycycline is given IV Calcium binding anf deposition in bone can discolour teeth Oral: colitis Myositis if long acting formulations are given IM Increasing resistance
63
How do fluoroquinalones work?
Bacteriocidal Concentration-dependent killing Inhibits DNA gyrase to prevent DNA supercoiling Abnormal DNA then gets degraded
64
Spectrum of fluoroquinalones
G-ve aerobes: Enterobacteriacea, Pseudomonas, Mycoplasma, Rickettsia, Ehrlicia. Limited g+ve aerobes (except Staph sp.), Limited anaerobes.
65
Distribution of fluoroquinalones
High lipid solubility hence reaches high concentration in the liver, spleen and kidneys, and moderate concentrations in the reproductive system, mammary glands, heart and muscles (very poor uptake in the central nervous system and eyes)
66
Excretion of fluoroquinolones
Urinary > biliary
67
Fluoroquinolone used in horses
Enrofloxacin
68
Cephalosporin used in horses
Ceftiofur
69
Action of cephalosporins
Bacteriocidal - inhibits cell wall synthesis Time dependent killing
70
Spectrum of cephalosporins
Broad spectrum; including Enterobacteriaeceae, anaerobes including Fusobacterium and clostridial disease, Pasteurella highly susceptible. Resistants include Bacteroides, Enterococcus, Rhodococcus, Pseudomonas
71
Metabolism of cephalosporins
Hydrolysed by the liver, excreted by the kidneys
72
When to use enrofloxacin in horses
G-ve aerobes or Staph species Osteomyelitis, respiratory tract, septic arthritis, URIs, cholangiohepatitis, pyoderma, cellulitis, internal abscesses Due to limited spectrum, generally needs polypharmacy
73
Use of ceftiofur in horses
Good intracellular and good against Corynebacterium hence good for internal abscesses. Labelled use is strictly for treatment of B-haemolytic Streptococcus species but is a good broad-spectrum (Strangles, pneumonia, abscesses, skin, UTIs, joints). Can combine with aminoglycosides for better G-ve action (peritonitis, cholangiohepatitis, septic arthritis) IVRP, joint infections (can use intra-articular)
74
What to be aware of when using enrofloxacin
Protected! Narrow spectrum – not a “stronger” antibiotic! Non-inflammatory arthropathy (foals) Desmitis/weakened tendons? Ataxia and neurological sign Tissue irritation – limited use in IVRP, never IM Oral ulceration (PO) Colitis
75
Things to be aware of when using ceftiofur
Protected! 3rd generation cephalosporin Colitis, diarrhoea Injection site discomfort
76
Which antimicrobials must never be used IV?
Procaine penicillin Doxycycline
77
What drug is gentamycin commonly used in conjunction with, and why?
Penicillin to cover gram positive as well, ceftiofur
78
By which routes can metronidazole be given?
Oral and rectal
79
What environments should TMPS never be used in?
Necrotic or pus
80
Which drug should TMPS never be given in conjunction with?
Alpha 2s
81
How do alpha-2 agonists work?
Act on alpha-2 adrenoreceptors Pre-synaptic inhibition of noradrenaline release Anaesthetic sparing
82
Commonly used alpha-2 agonists in horses
Xylazine - shortest acting (up to 20mins) Detomidine - most used (up to 40 mins) Romifidine - longest acting (up to 60 mins)
83
What drug are alpha-2 agonists commonly used in combination with?
An opioid - usually butorphanol
84
What do we need to be aware of before using alpha-2 agonists?
Cardiovascular depression and ileus - minimal Ataxia - xylazine most of all Should stay standing Variable sensitivities IV risks - avoid IA! ADH inhibition - diuresis

Equine I (21 decks)

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