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Veterinary Pharmacology > DRUGS FINAL > Flashcards

DRUGS FINAL Flashcards

1
Q

Neuroleptics (Tranquelizers)

A

Phenothiazines
1. Acepromazine
2. Chloropromazine
3. Propionylpromazine

Butyrophenones
1. Azaperone
2. Droperidol

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2
Q

Sedatohypnotics

A
  1. A2 AGONISTS
  2. A2 ANTAGONISTS
  3. Benzodiazepines
  4. Long acting BARBITURATE
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3
Q

Sedatohypnotics
A2 AGONISTS

A
  1. Xylazine
  2. Detomidine
  3. Dexmedetomidine
  4. Medetomidine
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4
Q

Sedatohypnotics
A2 ANTAGONISTS

A

A2 ANTAGONISTS
1. Atipamezole
2. Yohimbine

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5
Q

Sedatohypnotics
Benzodiazepines

A

Benzodiazepines
1. Diazepam
2. Midazolam
3. Alprazolam

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6
Q

Sedatohypnotics
Long acting BARBITURATE

A

Long acting BARBITURATE
1. Phenobarbital

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7
Q

A2 Agonist
Mechanism of action

A
  • Agonist of alpha-adrenoreceptor
  • On Post synaptic –>** Activates a1+a2** = Hypertension
  • On Pre synatic –> Only alpha 2 –> Hypotension
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8
Q

Alpha 2 agonist
Indications

A
  1. Sedation
  2. Analgesia
  3. For minor surgeries (ear or wound)
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9
Q

Alpha 2 agonist
Pharmacokinetics

A
  • Rapid absorbtion with relative quick onset of action (minuttes)
  • Good distribution, binds to plasmaproteins
  • Metabolism in Liver –> Not to liver patients
  • Excretion via Urine
  • Administration –> IM or IV
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10
Q

Alpha 2 agonist
Xylasine
Detomidine
Medetomidine

Can be given to which species?

A

Xylasine –> All domesticated animals
Detomidine –> Mainly in equines
Medetomidine –> Small animals

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11
Q

Alpha 2 Agonist
Side effects and contraindications

A
  • Hypertention then hypotension –> Not to cardiac patients
  • Vomiting/emesis in dog/cat
  • Increase blood glucose –> Not to diabetic patients
  • Tympany in Bovines (most sensitive to xylasine)
  • Sweatting in Equine
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12
Q

Which drug can reverse DETOMIDINE and DEXMEDETOMIDINE?

A

ATIPAMEZOLE

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13
Q

Which drug can reverse XYLASINE?

A

YOHIMBINE

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14
Q

Alpha 2 agonists
DOSAGES
Xylasine

A

Dog, Cat = 1-4 mg/kg IM,IV,SC
Horse = **0,5-1 mg/kg **
Cattle = 0,05 - 0,1 mg/kg

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15
Q

Alpha 2 agonists
DOSAGES
DEXMEDETOMIDINE

A

Dog = 10microg/kg
Cat = 40microg/kg
10-20 microg/kg for analgesia
IM, IV

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16
Q

Benzodiazepines
Mechanism of action

A
  • Stimulate GABA –> Result in opening of cl ion channel.
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17
Q

Benzodiazepines
Pharmacokinetics

A
  • Good oral absorbtion, im=delayed
  • Distribution is good –> Bind to plasmaproteins
  • Metabolism –> Enterohepatic circulation occurs (liver disease prolong activity)
  • Excretion via Kidney
  • Administration: IV or RECTALY
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18
Q

Benzodiazepines
DOSAGES
Diazepam

A

0,5-2 mg/kg IV

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19
Q

Benzodiazepines
Side effects and Contraindications

A
  • Hepatotoxicity
  • Contraindicated in cats (Liver damage long term diazepam)
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20
Q

Benzodiazepines
Antidote

A

FLUMAZENIL

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21
Q

Benzodiazepines
Indications

A
  • Sedation
  • Muscle relaxation
  • Premed
  • Antiepileptic
  • Phonophobia (Alprazolam)
  • (Diazepam = apetite stimulation)
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22
Q

Long acting Barbiturate
PHENOBARBITAL
Mechanism of action

A
  • Activates GABA a
  • Decrease Ca accumulation –> Therefore inhibiting the neurotransmitter release
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23
Q

Long acting Barbiturate
PHENOBARBITAL
Pharmacokinetics

A
  • Good PO absorbtion
  • IM causes tissue necrosis
  • Distribution to CNS + redistributes to adipose and muscle = It can accumulate –> Dont readminister!!
  • Metabolism in the LIVER, Induce CYP450 (not for liver patients)
  • Excretion via Urine
  • Administration = Mainly PO
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24
Q

Long acting Barbiturate
PHENOBARBITAL
Indication

A
  • Management of epilepsy
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25
Q

Long acting Barbiturate
PHENOBARBITAL
Side effects

A
  • Hepatotoxic
  • May cause respiratory depression
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26
Q

Long acting Barbiturate
PHENOBARBITAL
Dosage

A

PO
1-5 mg/kg BID

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27
Q

Neuroleptics (Tranquelizers)
What is it?

A

Tranquelizers are selective CNS depressants and can casue sedation, induce calming and decrease aggression!

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28
Q

Neuroleptics (Tranquelizers)
Phenothiazines
Mechanism of action

A
  • Antagonist of a-adrenoreceptor –> Hypotension and sedation
  • Antagonist of H1 receptor –> Antihistamine and antiemetic
  • Antagonist of dopamin receptor –> Antipsycotic, Increase Prolactin
  • Antagonist of serotonin receptor
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29
Q

Neuroleptics (Tranquelizers)
Phenothiazines
General effects

A
  • Antiemetics
  • Sedation
  • Potentiates analgesia
  • Antihistamine
  • Inhibit temp. regulation
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30
Q

Neuroleptics (Tranquelizers)
Phenothiazines
Pharmacokinetics

A
  • Poor oral absorbtion (buccal/rectal better)
  • Good distribution (cross BBB)
  • Slow onset of action
  • Metabolized in the liver
  • Slow elimination –>
  • Excretion by Urine
  • Not allwed in food producing animals due the long WP!
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31
Q

Neuroleptics (Tranquelizers)
Phenothiazines
Side effects

A
  • Hypotension causing collapse (boxers, bulldogs)
  • Penile prolaps –> EQ
  • Loss of thermoregulation
  • Tissue irritant
  • Increase Prolactin levels
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32
Q

Neuroleptics (Tranquelizers)
Phenothiazines
Contraindications

A
  • Not for pseudopregnant dogs
  • Not for cardiac or liver patients
  • Not in Dehydration/Hypovolaemia
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33
Q

Neuroleptics (Tranquelizers)
Phenothiazines
Indication

A
  • Calming + Sedation
  • Premedication
  • Acheave neurolept analgesia (Tranq+opioid)
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34
Q

Neuroleptics (Tranquelizers)
Phenothiazines
ACEPROMAZINE
Dosages

A

Dog =
* 1-2 mg/kg PO
* 0,2-0,3 mg/kg IV
Horse =
* 0,1-0,4 mg/kg PO
* 0,03-0,1 mg/kg IV

35
Q

Neuroleptics (Tranquelizers)
Butyrophenones
Mechanism of action

A

Antagonist/inhibitor of dopamin –> CNS
Azaperone, mainly in swine, IM
Not allowed IV

36
Q

Neuroleptics (Tranquelizers)
Butyrophenones
Side effects

A
  • Hypotension
  • Penile prolapse
  • Inhibition of thermoregulation
37
Q

Opioids
Active substances

A

Morphine
Codeine
Fentanyl
Tramadol
Butorphanol
Buprenorphine
Naloxone

38
Q

Opioids
In general

A

Opioids are originally from poppy plant Papaver Somniferum
Based on the structure in can be classified
* Alkaloids (Morphine, Codeine)
* Semisyntetic (Oxycodon, Buprenorphine)
* Synthetic (Fentanyl, Tramadol)

39
Q

Opioids
Mechanism of action

A
  • Spinal chord = Main site of action
  • In general opioids strongest analgesics, which is done by activating the decending pathways –> Inhibiting pain transmission in the dorsal horn and spine.
  • On the presynapse –> opioids inhibits Ca influx to inhibit neurotransmitter release.
  • On post synapse –> Causing hyperpolarization + inhibit the AP formation
  • Opioids binds to 3 main receptors
    1. Mu = In spine and synaptic region –> Inhibit respiratory center –> Respiratory depression
    2. Kappa = Only spine
    3. Delta = Spine

Kappa and Delta = Causes sedation and analgesia*

40
Q

Opioids
Opioid Agonists Antagonists

A
  • Agonist: Act on the Mu receptor
    1. Morphine
    2. Codeine
    3. Fentanyl
    4. Tramadol
  • Antagonist:
    1. Naloxone

Partial agonist:
1. Buprenorphine

Mixed agonists-antagonists:
1. Butorphanol = agonist on kapa, antagonist on Opioids
.

41
Q

Opioids
Pharmacokinetics

A

ABSORBTION = Good
- Oral administration –> First pass effect decrease F(bioavailability) =** Injetions is better (IM,IV)**
- Fentanyl can be absorbed through skin with **transdermal patch, **(3days)

DISTRIBUTION= Good
- Remmember morphine 30 min wait before effect, onset.
- Duration of action
* Morphine = 3-4hours
* Buprenorphine = 6-8 hours (up to 12hours)
* Butorphanol = 3-4 hours**

METABOLISM = Intensive metabolism in LIVER
EXCRETION via KIDNEY and URINE
Administration: IM, IV best for Bioavailability

42
Q

Opioids
Side Effects

A
  1. Respiratory depression
  2. Morphine = Histamine release (Acepromazine to counter)
  3. Emesis (Induce vomit with Acepromacine)
  4. Bradycardia
  5. Exitation (Horses and cats)
  6. Obstipation
43
Q

OPIOIDS
Indication

A
  1. Analgesia
  2. Sedation
  3. Antitussive
  4. Anti diarrhoeal (Loperamide)
  5. Emesis
44
Q

Opioids
Combinations

A
  1. Phenothiazines = Neurolept analgesia
  2. Benzodiazepines = Ataranalgesia
45
Q

Opioids
DOSAGES
Morphine

A

Dog = **0,3-0,8 **mg/kg
Cat + Horse = **0,1 **mg/kg

46
Q

Opioids
DOSAGES
Fentanyl

A

Most patients
* 1-5 microgram/kg Dog and Cat IV
* 6-8 microgram/kg Horse

47
Q

Inhalational Anaesthetics
Active Substances

A

1. Isoflurane
2. Sevoflurane
3. Halothane
4. Desflurane

Acts as general anaestehtics

48
Q

Inhalational Anaesthetics
Classified

A

ORGANIC
* Haogenated = Liquid
1. Isoflurane
2. Sevoflurane
3. Halothane
* Non-Halogenated
1. Diethyleter

INORGANIC
1. Xenon Gass

49
Q

Inhalational Anaesthetics
Mechanism of action

A

GABA a Allosteric Agonist = Neurotransmitter release inhibition.

50
Q

Inhalational Anaesthetics
Effects

A

1. Loss of conciousness
2. Muscle relaxation

But NO analgesic –> Comb w/ opioids –> Prolonged effect

51
Q

Inhalational Anaesthetics
Indications

A
  1. Induction
  2. Maintenance
  3. Anticonvulsant
52
Q

Inhalational Anaesthetics
Pharmacokinetics

A

Inhaled anaestathics
Good vaporization
Good blood gass distribution
Good lipid solubility in brain (Oil:gass distribution)
–> Too high lipid solubility = Prolonged effect

53
Q

Inhalational Anaesthetics
Side effects

A
  1. Cardiovascular depression
  2. Respiratory depression
  3. (Isoflurane irritetes mucosa)
54
Q

Inhalational Anaesthetics
Contraindications

A
  1. Young patients
    **2. Old patients
    **3. Pregnant
  2. Lactating
  3. Those proned to** Malignant hypothermia**
  4. METHOXYFLURANE = Nephrotoxic in reptiles
  5. HALOTHANE is carcinogenic and Nephrotoxic banned in EU)
55
Q

Injectable Anaesthetics
Active substances

What do they cause

A

BARBITURATES
* Pentobarbital
* Thiopental
Propofol
NMDA antagonists
* Ketamin
* Tiletamin
STEROID ANAESTHETICS
* Alphaxalone
* Alphadolone

They cause muscle relaxation + loss of conciousness BUT no analgesia. –> Combined with opioids for balanced anaestehsia

56
Q

Injectable Anaesthetics
Barbiturates
Mechanism of action

A

Allostere GABA a agonist –> Inhibit neurotransmitter release

57
Q

Injectable Anaesthetics
Barbiturates
Pharmacokinetics

A
  • IV administration ONLY –> Rapid effect
  • IM cause tissue irritation + necrosis
  • DISTRIBUTION = Lipophillic, cross bariers (BBB + placental)
  • Redistribution occur to muscle and fat –> Accumulates = No readministration.
  • Metabolism in the LIVER = Carefull with liver patients
  • Excretion by KIDNEY and URINE , Very slow (days)
58
Q

Injectable Anaesthetics
Barbiturates
Side effects

A

NARROW TI
1. Respiratory and cardiovascular depression
2. Tissue irritation
3. Excitation (especially in Eq and Fe)
4. Grayhounds are sensitive

59
Q

Injectable Anaesthetics
Barbiturates
Indications

A
  1. General anaesthesia (with opioids)
  2. Phenobarbital –> Epilepsy and euthanasia
60
Q

Injectable Anaesthetics
Propofol
Mechanism of action

A

Allosteric and Orthosteric GABA A agonist

61
Q

Injectable Anaesthetics
Propofol
Dosage

A
  • IV 6-8mg/kg (withouth premed)
  • IV 3-4 mg/kg (With premed)
62
Q

Injectable Anaesthetics
Propofol
Pharmacokinetics

A
  • Given IV, but is a microemulsion = Give SLOWLY
  • Cross BBB and Placental barrier
  • Metabolism in the LIVER, despite this with carefull dosage can be given to liver patients (Intestines takes over)
  • Extretion in URINE
63
Q

Injectable Anaesthetics
Propofol
Side effects

A
  1. Apnoe, if quick administration
  2. Cardiac depression = Contraindicated in cardiac patients
  3. Vomiting
64
Q

Injectable Anaesthetics
Propofol
Indication

A
  1. Induction and maintenance of anaesthetics
    (Combination with opioids)
65
Q

Injectable Anaesthetics
NMDAr antagonists
Active ingredients

A

Ketamine and Tiiletamin

66
Q

Injectable Anaesthetics
NMDAr antagonists
Mechanism of action

A
  • Antagonize NMDAr which is responsible for pain sensation.
  • Only injectable with analgesic effect (reduces pain sens)
  • But does NOT provide muscle relaxation, instead muscle RIGIDITY.
  • Use with A2 agonist, Benzodiazepines (Diazepam) + Propofol
67
Q

Injectable Anaesthetics
NMDAr antagonists
Pharmacokinetics

A
  • IV administration (IM=tissue irritant)
  • Metabolism in the LIVER
  • Excreted by KIDNEYS = Not for kidney failure in cats, because active form excreted in cats.
68
Q

Injectable Anaesthetics
NMDAr antagonists
Side effects

A
  1. Ketamin cause CATALEPSY
  2. Respiratory depression
  3. Salivation
  4. Increased CO and BP
  5. Increase ICP = Not in head injury
  6. Contraindicated in LIVER and KIDNEY patients.
69
Q

Injectable Anaesthetics
NMDAr antagonists
Indication

A
  • Induction and maintenance of anaesthesia in combinations ONLY
  • Safe in DOGS and HORSES ONLY - Must be in combinations
70
Q

Injectable Anaesthetics
NMDAr antagonists
KETAMINE dosage

A

Horse IV 0,4-0,8 mg/kg/hr
Dog IV (IM) 5-10mg/kg in anaesthesia comb

71
Q

Injectable Anaesthetics
Steroid Anaesthetics
Active substances

A
  1. Althresin = Alphaxalon
  2. Alfadalone
72
Q

Injectable Anaesthetics
Steroid Anaesthetics
Pharmacokinetics

A
  • In combinations with opioids for analgesia
  • Cause histamine release
  • Crosses BBB
  • Metabolized in the LIVER
  • Excreted by KIDNEY + URINE
  • Fast IV onset
73
Q

Injectable Anaesthetics
Steroid Anaesthetics
Side effects

A
  1. Cardiovascular depression
  2. Histamine release = Allergy
74
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Active substances

A

Digoxin
Pimobendan

75
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Cardiotonics in General

A
  • Used to treat CHRONIC HEART FAILURE
  • In case of heart failure there is decreased performance –> Want to improve
  • Cardiotonics such as Digitalis Glycosides used to increase CONTRACTILLITY
76
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Phosphodiesterase inhibitors in General

A

Phosphodiesterase inhibitors like PIMOBENDAN can increase contractillity as well as decrease preload and afterlode

77
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Over all Cardiotonics …..

A

Have a direct cardiac action by neccessary CO + improving RBF allowing for water + Na secretion.
Also increases vagal tone = causing BRADYCARDIA

78
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES –> DIGOXIN
Mechanism of action

A
  • Inhibits the Na/K ATPase pump, which is responsible for Na influx and K efflux.
  • Result in high Ca concentrations and hypokalaemia
79
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES –> DIGOXIN
Pharmacokinetics

A
  • Absorbtion = Orally (6day + 1day off)
  • Distribution = High protein binding ability –> Result in drug interactions
  • Accummulates in myocytes
  • Excreted via KIDNEY and URINE
80
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES –> DIGOXIN
Side effects and contra indications

A

NARROW TI
1. Toxicosis
2. Hypokelaemia
3. Bradycardia
4. GI signs - Vomiting

Contraindication: Outflow obstruction caused by Stenosis or HCM

81
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES –> DIGOXIN
Indication

A

Supraventricular tachyarrythmias

82
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
PDE Inhibitors –> PIMOBENDAN
Mechanism of action

A
  1. Phosphodiesterase inhibition –> cAMP accumulation in myocardial cells –> Increase Ca concentration –> Positive inotropic/increase contrctillity
  2. PDE Inhibition –> Atrial and venous dilation –> Decrease Pre-afterload
83
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
PDE Inhibitors –> PIMOBENDAN
Pharmacokinetics

A
  • Per Os without feed (reduces F)
  • Extensive protein binding –> Drug interactions
  • Excreted via KIDNEY and URINE
84
Q

Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
PDE Inhibitors –> PIMOBENDAN
Side effects

A

Rare, but GI signs like nausea and vomiting

Veterinary Pharmacology (21 decks)

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