DRUGS FINAL Flashcards
(84 cards)
1
Q
Neuroleptics (Tranquelizers)
A
Phenothiazines
1. Acepromazine
2. Chloropromazine
3. Propionylpromazine
Butyrophenones
1. Azaperone
2. Droperidol
2
Q
Sedatohypnotics
A
- A2 AGONISTS
- A2 ANTAGONISTS
- Benzodiazepines
- Long acting BARBITURATE
3
Q
Sedatohypnotics
A2 AGONISTS
A
- Xylazine
- Detomidine
- Dexmedetomidine
- Medetomidine
4
Q
Sedatohypnotics
A2 ANTAGONISTS
A
A2 ANTAGONISTS
1. Atipamezole
2. Yohimbine
5
Q
Sedatohypnotics
Benzodiazepines
A
Benzodiazepines
1. Diazepam
2. Midazolam
3. Alprazolam
6
Q
Sedatohypnotics
Long acting BARBITURATE
A
Long acting BARBITURATE
1. Phenobarbital
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
8
Q
Alpha 2 agonist
Indications
A
- Sedation
- Analgesia
- For minor surgeries (ear or wound)
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
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
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
12
Q
Which drug can reverse DETOMIDINE and DEXMEDETOMIDINE?
A
ATIPAMEZOLE
13
Q
Which drug can reverse XYLASINE?
A
YOHIMBINE
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
15
Q
Alpha 2 agonists
DOSAGES
DEXMEDETOMIDINE
A
Dog = 10microg/kg
Cat = 40microg/kg
10-20 microg/kg for analgesia
IM, IV
16
Q
Benzodiazepines
Mechanism of action
A
- Stimulate GABA –> Result in opening of cl ion channel.
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
18
Q
Benzodiazepines
DOSAGES
Diazepam
A
0,5-2 mg/kg IV
19
Q
Benzodiazepines
Side effects and Contraindications
A
- Hepatotoxicity
- Contraindicated in cats (Liver damage long term diazepam)
20
Q
Benzodiazepines
Antidote
A
FLUMAZENIL
21
Q
Benzodiazepines
Indications
A
- Sedation
- Muscle relaxation
- Premed
- Antiepileptic
- Phonophobia (Alprazolam)
- (Diazepam = apetite stimulation)
22
Q
Long acting Barbiturate
PHENOBARBITAL
Mechanism of action
A
- Activates GABA a
- Decrease Ca accumulation –> Therefore inhibiting the neurotransmitter release
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
24
Q
Long acting Barbiturate
PHENOBARBITAL
Indication
A
- Management of epilepsy
25
Long acting Barbiturate
PHENOBARBITAL
Side effects
* Hepatotoxic
* May cause respiratory depression
26
Long acting Barbiturate
PHENOBARBITAL
Dosage
PO
1-5 mg/kg BID
27
Neuroleptics (Tranquelizers)
What is it?
Tranquelizers are selective CNS depressants and can casue sedation, induce calming and decrease aggression!
28
Neuroleptics (Tranquelizers)
Phenothiazines
Mechanism of action
* 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**
29
Neuroleptics (Tranquelizers)
Phenothiazines
General effects
* Antiemetics
* Sedation
* Potentiates analgesia
* Antihistamine
* Inhibit temp. regulation
30
Neuroleptics (Tranquelizers)
Phenothiazines
Pharmacokinetics
* **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!**
31
Neuroleptics (Tranquelizers)
Phenothiazines
Side effects
* Hypotension causing collapse (boxers, bulldogs)
* Penile prolaps --> EQ
* Loss of thermoregulation
* Tissue irritant
* Increase Prolactin levels
32
Neuroleptics (Tranquelizers)
Phenothiazines
Contraindications
* Not for **pseudopregnant dogs**
* Not for **cardiac** or **liver patients**
* Not in **Dehydration**/Hypovolaemia
33
Neuroleptics (Tranquelizers)
Phenothiazines
Indication
* Calming + Sedation
* Premedication
* Acheave neurolept analgesia (Tranq+opioid)
34
Neuroleptics (Tranquelizers)
Phenothiazines
ACEPROMAZINE
Dosages
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
Neuroleptics (Tranquelizers)
Butyrophenones
Mechanism of action
Antagonist/inhibitor of dopamin --> CNS
Azaperone, mainly in swine, IM
Not allowed IV
36
Neuroleptics (Tranquelizers)
Butyrophenones
Side effects
* Hypotension
* Penile prolapse
* Inhibition of thermoregulation
37
Opioids
Active substances
**Morphine**
Codeine
**Fentanyl**
**Tramadol**
**Butorphanol**
**Buprenorphine**
**Naloxone**
38
Opioids
In general
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
Opioids
Mechanism of action
* **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
Opioids
Opioid Agonists Antagonists
- **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
Opioids
Pharmacokinetics
**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
Opioids
Side Effects
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
OPIOIDS
Indication
1. Analgesia
2. Sedation
3. Antitussive
4. Anti diarrhoeal (Loperamide)
5. Emesis
44
Opioids
Combinations
1. **Phenothiazines** = **Neurolept** analgesia
2. **Benzodiazepines** = **Ataranalgesia**
45
Opioids
DOSAGES
Morphine
Dog = **0,3-0,8 **mg/kg
Cat + Horse = **0,1 **mg/kg
46
Opioids
DOSAGES
Fentanyl
Most patients
* **1-5 microgram/kg Dog** and **Cat** **IV**
* **6-8** **microgram**/kg **Horse**
47
Inhalational Anaesthetics
Active Substances
**1. Isoflurane
2. Sevoflurane
3. Halothane
4. Desflurane**
| Acts as general anaestehtics
48
Inhalational Anaesthetics
Classified
ORGANIC
* **Haogenated** = Liquid
1. Isoflurane
2. Sevoflurane
3. Halothane
*** Non-Halogenated**
1. Diethyleter
INORGANIC
**1. Xenon Gass**
49
Inhalational Anaesthetics
Mechanism of action
**GABA a** Allosteric Agonist = Neurotransmitter release inhibition.
50
Inhalational Anaesthetics
Effects
**1. Loss of conciousness
2. Muscle relaxation**
But **NO** **analgesic** --> Comb w/ opioids --> Prolonged effect
51
Inhalational Anaesthetics
Indications
1. Induction
2. Maintenance
3. Anticonvulsant
52
Inhalational Anaesthetics
Pharmacokinetics
Inhaled anaestathics
Good vaporization
Good blood gass distribution
Good lipid solubility in brain (Oil:gass distribution)
--> Too high lipid solubility = Prolonged effect
53
Inhalational Anaesthetics
Side effects
1. Cardiovascular depression
2. Respiratory depression
3. (Isoflurane irritetes mucosa)
54
Inhalational Anaesthetics
Contraindications
1. **Young** **patients**
**2. Old patients
**3. **Pregnant**
4. **Lactating**
5. Those proned to** Malignant hypothermia**
6. METHOXYFLURANE = **Nephrotoxic** in **reptiles**
7. HALOTHANE is **carcinogenic** and **Nephrotoxic** banned in EU)
55
Injectable Anaesthetics
Active substances
| What do they cause
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
Injectable Anaesthetics
Barbiturates
Mechanism of action
Allostere GABA a agonist --> Inhibit neurotransmitter release
57
Injectable Anaesthetics
Barbiturates
Pharmacokinetics
* **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
Injectable Anaesthetics
Barbiturates
Side effects
NARROW TI
1. Respiratory and cardiovascular depression
2. Tissue irritation
3. Excitation (especially in Eq and Fe)
4. Grayhounds are sensitive
59
Injectable Anaesthetics
Barbiturates
Indications
1. General anaesthesia (with opioids)
2. Phenobarbital --> Epilepsy and euthanasia
60
Injectable Anaesthetics
Propofol
Mechanism of action
Allosteric and Orthosteric GABA A agonist
61
Injectable Anaesthetics
Propofol
Dosage
* IV 6-8mg/kg (withouth premed)
* IV 3-4 mg/kg (With premed)
62
Injectable Anaesthetics
Propofol
Pharmacokinetics
* 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
Injectable Anaesthetics
Propofol
Side effects
1. Apnoe, if quick administration
2. Cardiac depression = Contraindicated in cardiac patients
3. Vomiting
64
Injectable Anaesthetics
Propofol
Indication
1. **Induction** and **maintenance** of anaesthetics
(Combination with **opioids**)
65
Injectable Anaesthetics
NMDAr antagonists
Active ingredients
**Ketamine** and **Tiiletamin**
66
Injectable Anaesthetics
NMDAr antagonists
Mechanism of action
* 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
Injectable Anaesthetics
NMDAr antagonists
Pharmacokinetics
* 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
Injectable Anaesthetics
NMDAr antagonists
Side effects
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
Injectable Anaesthetics
NMDAr antagonists
Indication
* **Induction** and **maintenance** of anaesthesia in **combinations ONLY**
* Safe in **DOGS and HORSES ONLY** - Must be in combinations
70
Injectable Anaesthetics
NMDAr antagonists
KETAMINE dosage
Horse IV 0,4-0,8 mg/kg/hr
Dog IV (IM) 5-10mg/kg in anaesthesia comb
71
Injectable Anaesthetics
Steroid Anaesthetics
Active substances
1. Althresin = Alphaxalon
2. Alfadalone
72
Injectable Anaesthetics
Steroid Anaesthetics
Pharmacokinetics
* In combinations with opioids for analgesia
* Cause histamine release
* Crosses BBB
* Metabolized in the LIVER
* Excreted by KIDNEY + URINE
* Fast IV onset
73
Injectable Anaesthetics
Steroid Anaesthetics
Side effects
1. Cardiovascular depression
2. Histamine release = Allergy
74
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Active substances
Digoxin
Pimobendan
75
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Cardiotonics in General
* 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
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Phosphodiesterase inhibitors in General
Phosphodiesterase inhibitors like **PIMOBENDAN** can **increase contractillity** as well as **decrease preload** and **afterlode**
77
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
Over all Cardiotonics .....
Have a **direct** cardiac action by neccessary CO + **improving RBF** allowing for **water + Na secretion**.
Also **increases vagal tone** = causing **BRADYCARDIA**
78
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES --> DIGOXIN
Mechanism of action
* **Inhibits the Na/K ATPase pump**, which is responsible for **Na influx** and **K efflux.**
* Result in **high Ca concentrations** and **hypokalaemia**
79
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES --> DIGOXIN
Pharmacokinetics
* Absorbtion = **Orally** (6day + 1day off)
* Distribution = High **protein binding** ability --> Result in **drug interactions**
* Accummulates in **myocytes**
* Excreted via **KIDNEY** and **URINE**
80
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES --> DIGOXIN
Side effects and contra indications
NARROW TI
1. Toxicosis
2. Hypokelaemia
3. Bradycardia
4. GI signs - Vomiting
Contraindication: Outflow obstruction caused by Stenosis or HCM
81
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
DIGITALIS GLYCOSIDES --> DIGOXIN
Indication
Supraventricular tachyarrythmias
82
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
PDE Inhibitors --> PIMOBENDAN
Mechanism of action
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
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
PDE Inhibitors --> PIMOBENDAN
Pharmacokinetics
* Per Os **without feed** (reduces F)
* Extensive protein binding --> Drug interactions
* Excreted via KIDNEY and URINE
84
Cardiotonics (Digitalis glycosides + Phosphodiesterase inhibitors)
PDE Inhibitors --> PIMOBENDAN
Side effects
**Rare**, but **GI signs** like **nausea** and **vomiting**
