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Pharma midterm 1 > Lecture 9-11 - CNS depressant > Flashcards

Lecture 9-11 - CNS depressant Flashcards

1
Q

What are organotropic drugs?

A

drugs that work on body organs

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2
Q

What are etiotropic drugs?

A

drugs that acts on parasites, microber, bacteria

tumor cells

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3
Q

What are the criterias for neurotransmitters?

A
  • must be present in the nerve terminals
  • must be relaesed on nerve stimulation
  • exogenous application of the substance must mimic nerve stimulation
  • it should be synthesized and stored in neurons
  • it is inactivated or eliminated quickly
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4
Q

What are the main excitatory amino acids and their effect

A

glutamate and aspartate

effect: depolarization (increases transmission)

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5
Q

What are the main inhibitory amino acids and their effect?

A

Glycine and GABA

Effect: hyperpolarization (stabilization of post synaptic membrane)

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6
Q

What transmitter belongs to the choline esters and what is the function?

A

Acetylcholine

(hyper)- or depolarisation

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7
Q

What neurotransmitters belong to the monoamines?

A

noradrenaline

adrenaline

dopamine

serotonin

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8
Q

what is the effect of noradrenaline?

A

postsynaptic alpha and beta

mood

blood pressure

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9
Q

what is the effect of adrenaline?

A

locomotor activity

body temperature

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10
Q

what is the effect of dopamine?

A

behaviour, locomotor activity

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11
Q

What is the effect of serotoning?

A

prolactin secretion decreases

vomiting

sleep

body temperature

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12
Q

What neurotransmitters belongs to the group of neuopeptides?

A

encephalins

endorphines

substance-P

neurokinins

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13
Q

What is the effect of neuropeptides?

A

analgesia

respiratory and circulatory depression

euphoria

dysphoria

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14
Q

Where can acethylcholine be found?

A

widely distributed throughout the CNS

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15
Q

What receptors does Ach bind to and what is the consequence?

A

M1 receptors

closes: K+- Ca2+-, Cl–ion channels

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16
Q

What happens to the cells when Ach binds?

A

depending on the type it will either depolarize or hyperpolarize

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17
Q

How is Ach inactivated?

A

hydrolysis

Ach-esterase

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18
Q

Where can Norephinephrine be found?

A

uneven distributions of the CNS

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19
Q

What receptors is norephinephrine binding to?

A

Receptor alpha (a1-Gq -, A2Gi)

Beta (Gs)

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20
Q

What is the task of a2 receptors?

A

important in control of sleep and wakefulness, mood and emotional behaviour, temperature

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21
Q

What dopamine receptors do we have?

A

D1

D5 (Gs)

D2

D3

D4 (Gi)

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22
Q

Where can dopamin be found in largest concentrations?

A

basal ganglia and limbic system

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23
Q

What effect does dopamine excert?

A

inhibitory effect

fine control of movement

disturbances of behaviour

hypothalamic-pituitary functions

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24
Q

What effect is excerted by serotonin?

A

strong inhibitory effect

hyperpolarization by increasing K+ and Na+ conductance

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25
Q

What is the result of serotonin stimualtion?

A

inhibits pain pathways in the spinal cord

helps ccontrol of behaviroual mood

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26
Q

what is the proposed regulatory function of serotonin?

A

sleep and wakefulness

mood and emotion

temperature

appetite

neuroendrocrine control

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27
Q

what effect does serotonin have on other neurotransmitters?

A

inhibits the release

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28
Q

What histamine receptors do we have?

A

H1 (Gq)

H2 (Gs)

H3

H4 (Gi)

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29
Q

where can histamine mostly be found?

A

posterior hypothalamus

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30
Q

what actions are histamin involved with?

A

regulation of arousal

temperature

and

vascular dynamics

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31
Q

What is the effect of histamin on other neurotransmitters?

A

decreases

Ach

5-HT

NA release

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32
Q

Where can glutamate and aspartate be found?

A

uniquely high concentration in brain

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33
Q

Where is GABA found

A

widely distributed in the CNS

highest concentration in

  • basal ganglia
  • hippocampus
  • cerebellum
  • spinal cord
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34
Q

What GABA receptors do we have and what is the action?

A

GABA a and b

facilitate Cl- and K+ ion transport, respectively

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35
Q

What is the action of glycine?

A

inhibits transmission between spinal interneurons and motor neurons

action is restricted to the spinal cord

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36
Q

What are the major purposes of the applications of drugs acting on CNS?

A
  • Prevention of seizures
  • increase well-being
  • alteration of behaviour
  • improvement of animal-human interaction
  • induction sleep
  • induction anaesthesia
  • induction arousal
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37
Q

What are analeptics?

A

CNS stimulants

convulsants and respiratory stimulants

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38
Q

How do we classify CNS stimulants based on their site of action?

A

cortical

medullar

spinal

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39
Q

give some examples of drugs acting cortical

A

xanthines - coffein

cocain

amphetamines

psychotomimetics - LSD

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40
Q

give some exmaples of drugs that act medullar

A

xanthines- coffein

pentetrazol

doxapram

picrotoxin

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41
Q

give example of a drug that acts spinal

A

strychine

  • toxic substance, motory, sensory activity stimulator
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42
Q

Doxapram is an example of a…?

A

respiratory stimulant

  • short acting

given IV to treat acute resp failure

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43
Q

strychnine is an example of…?

A

miscellaneous convulsant

it is the antagonis of glycine, increases reflex excitablity of SC

no clinical use

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44
Q

what is picrotoxin an example of?

A

miscellaneous convulsant

non competitive antagonist of GABA

clinical use as respiratory stimulant

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45
Q

Name some psychotomimetic drugs

A

LSD

MDMA

Mescaline

Psilocybin

Phencyclidine

amphetamine

cocaine

methylxanthines

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46
Q

What is the mode of action of LSD?

A

agonist at 5-HT receptors

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47
Q

what is the mode of action of MDMA?

A

releases 5-HT and blocks reuptake

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48
Q

What is an example of methylxanthines?

A

caffein

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49
Q

What are the four identifiable actions in vitro of caffein?

A
  1. adenosine receptor blockade
  2. phosphodiesterase inhibition
  3. action at Ca++ channels to increase entry of Ca++ into cells
  4. binding to GABA receptors at the benzodiazepine site
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50
Q

What is the task of phosphodiesterase?

A

responsible for the breakdown of cAMP

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51
Q

What is the primary action of caffein?

A

direct action of blocking adenosine receptors

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52
Q

What is the general effect of adenosine that caffein will block?

A

inhibit neural activity

so the caffein will increase neural activity

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53
Q

What will the caffeins antagonism of adenosine action on A2a receptor in the globus pallidus cause?

A

decreases release of GABA (inhibitory neurotransmitter)

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54
Q

What is the effect of benzodiazepine and what effect can caffein have on this?

A

benzodiazepines acts by enhancing the effect of GABA on GABAa receptors

caffein has an opposite effect by inhibiting GABA release

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55
Q

Why does caffein cause vasoconstriction?

A

adenosine A2 receptors are prominent in endothelial cells, resulting in vasodilation - caffein counteracts adenosine effecct

56
Q

What is the effect of methylxanthines on the heart?

A

postive ionotropic and chronotropic effect

57
Q

what is the relationship between methylxanthines and peptic ulcers?

A

methylxanthines stimulate peptic acid secretion

58
Q

How are analeptics classified?

A

Central analeptics

periferal analeptics

mixed analeptics

59
Q

What are some example of central analeptics?

A

methyxanthins

picrotoxin

60
Q

What are some examples of periferal analeptics

A
  • cropropramide:crotetamied =prethcamid
    • mixture of agents
    • clinically available
  • lobelin
61
Q

what are some mixed analeptics?

A

doxapram

nicetamid, CO2, campho

62
Q

How are the convulsants and respiratory stimulating drugs, doxapram, picrotoxin and strychnine used?

A

Doxapram: short-acting respiratory stimulant, used in acute respiratory failure

Strychnine: convulsant poison, acts on spinal cord by blocking receptors for the inhibitory transmitter glycine

picrotoxin: acts as GABAa antagonis, blocks ion channels

63
Q

What are some things to consider about CNS depressants?

A

the nature of their effects

the site of action

the selectivity of the effect

the mode of action

64
Q

What are the different categories based upon the nature of the effect of the CNS depressants?

A

Tranquilliser sedatives

Hypnosedatives

Analgesics

General anaesthetics

Anticonvulsants

Central muscle relaxants

65
Q

What are the three major tranquilliser?

A
  1. phentothiazine derivatives
  2. butyrophenones
  3. (Rauwolfia alkaloids - reserpine)
66
Q

What are the phentothiazine derivative drugs?

A

propiopromazine

acepromazine

chlorpromazine

prometazine

67
Q

Butyrophenones drugs

A

Azaperone

(haloperidol, droperidol, fluanisone)

68
Q

What are the 4 groupings of hypnosedatives?

A
  1. alpha2-agonist
  2. benzodiazepines
  3. propandiol-derivatives
  4. other compounds
69
Q

Name som drugs that are alpha2-agonists

A

xylazine

medetomidinie, dexmedetomidine

romifidine, detomidine, anxiolytics

70
Q

name som drugs that belong to Benzodiazepines

A

diazepam

chloridiazepoxide

71
Q

Name a drug that belong to propandiol-derivatives

A

meprobamate

72
Q

nae some other compounds that are hypnosedatives

A

barbiturates - long acting

alcohols

aldehydes

Br- and Mg2+ salts

73
Q

What are psychotherpeutic drugs

A

compounds that influence behaviour, mood and emotional reactions

74
Q

what are some psychotherapeatic drug categories?

A

anxiolytic drugs, sedative-hypnotic drugs

antipsychotic drugs

antidepressant drugs

75
Q

What is the receptoral effects of tranquillisers on dopaminergic receptors?

A

D2 antagonists –> antipsychotic effect

antimetic effect

increase in prolactin

parkinson-syndrome

76
Q

Phenothiazine derivatives are ?

A

tranquillisers

77
Q

How does tranquillisers act on the a-adrenoceptor

A

antagonistic

hypo tension

sedation?

78
Q

what is the effect of tranquillisers on the muscarinic receptor?

A

antagonistic

mainly side effects

79
Q

What is the effect of tranquillisers on H1-receptors?

A

antagonistic

sedation, antiemetic effect

80
Q

what is the effect of tranquillisers on 5HT-receptors

A

antagonistic

enhancement of several effects

81
Q

what are the pharmacological effects of phentothiazine derivatives?

A

potentation - sedatives, hypnotics, analgesic

vegetative tone decreases with increased relative parasympathetic tone

circulation

central antiemetic effect

regulation of body temperature

82
Q

What are the uses of phenothiazines?

A

calming, sedation

muscle relaxation

premediaction before general anaesthesia

83
Q

What are the side effects-contraindication of phenothiazines?

A

hypotention –> collapse, tissue irritation, allergy

horses: excitation, penile prolaps
pets: thrid eyelid prolaps

prolactin increases

FSH,LH decrease

ADH and oxytocin decreases

epilepsy, extrapyramidal symptoms

84
Q

How is the dosage of tranquillisers?

A

IV

IM

Po

range: 0,5-5 mg/kg

85
Q

How is chloropromozine as a tranquilliser?

A
  • side effects- frequently
  • paradox reaction in horses
    • cycli ataxia reaction with excitation hypotension and tachycardia
    • rarely in other animals
  • tissue irritation
  • allergy
86
Q

how is propriopromazine as an tranquilliser?

A

reliable, less side effects

87
Q

How is acepromazine as an tranquilliser?

A

more efficacious than chloropromazine

less side effects

good oral bioavailability

halothane hyperthermia

arrythmogenicity

88
Q

What is prometazine as a tranquilliser?

A

less potent tranquillizer

increased antihistaminic

anti-5-HT effect

89
Q

How are butirophenones as tranquillisers?

A
  • more potent than phentothiazines - analgesic effect
  • in the CNS
    • dopamine inhibition
    • NA inhibition
    • anticholinergic effect
90
Q

what are the side effect-contradiction of butrophenones?

A

transient salivation or panting

hypotension, respiratory stim.

boar penile prolaps

should be avoided in cold conditions

91
Q

what are the most characterisitic effects of sedative-hypnotics?

A

sedative effect

anxyolytic effect

hypnotic effect - induce or maintain sleep

muscle relaxation

anticonvulsive

92
Q

what are the alpha2-agonists

A

xylazine

detomidine

dex/medetomidine

romifidine

93
Q

what are the pharmacological effects of alpha2-agonists?

A

postsynaptic

  • a2 and a1
    • vasoconstriction
      • transient hypertension

presynaptic

  • a2
    • vasoconstriction
      • bradycardia
    • vagus bradycardia
      • hypotension
94
Q

Alpha2-agonists pharmacologocal effects

activation of postsynaptic receptorss

A

vasoconstriction

transient hypertension

activation of baroreceptor

vagyllymediated bradycardia

95
Q

ALPHA2-AGONISTS PHARMACOLOGOCAL EFFECTS

activation of presynaptic a2-receptors inhibits the release of NA

A

suppressed vasomotor tone - hypotension

analgesia and sedation

reduced motoractivity - recumbency

vagal bradycardia

96
Q

ALPHA2-AGONISTS PHARMACOLOGOCAL EFFECTS

further effects due to activation of a2-receptors

A

GI SM relaxation

mydriasis, introcular pressure decreases

salivation decreases

release of insulin, renin and ADH decreases

ACTH increases

97
Q

What are the side effects of Alfa2-adrenoreceptors in the different animals?

98
Q

Pharmacokinetics of Alfa2-agonists

99
Q

What type of drug is xylazine?

A

sedative-analgesic drug with depressed motor activity

100
Q

what are the side effects of xylazine?

A
  • emesis and vomiting in cats and dog
  • bradycardia, malignant arrhytmias
  • sweating in horses
  • ecbolicaction - used as a contradiction in late pregnancies
  • tympani in ruminants
101
Q

What is the dose in

horses

cattle

dogs

cats

A

Horses:

  • 2-3mg IM
  • 0,5-10, mg/kg IV

cattle

  • 0,05-0,2 mg/kg IM

Dog

  • 1-2mg/kg IM

Cat

  • 3mg/kg IM
102
Q

What type of drug is detomidine?

A

a Sedative-analgesic drug more potent than xylazine

103
Q

For what animal is detomidine used?

104
Q

why is detomidine a good drug for horses?

A

it does not cause loss of consciousness, and the duration of action is dose dependent

the horse can remain standing

105
Q

What are the side effects of detomidine?

A

hypertension

bradycardia

respiratory depression

diuresis

hypothermia

sweating

snoring

tremor

106
Q

How is detomidine used?

A

alone or in combination with ketamine. thiopentone, opioid drugs

107
Q

what is the dosage of detomidine?

A

10-80 microgram/kg IM or IV

40microgrm/kg PO

108
Q

Why is medetomidine and dexmedetomidine used?

A

it has similar effects as xylazine but is more reliable and safer

109
Q

what species are best for Dex/medetomidine?

A

cats and dogs

110
Q

what is the duration of action on medetomidine and dexmetomidine?

A

Medetomidine

  • sedation: 1-3h
  • analgesia: 5-15min

Dexmedetomidine

  • sedation: 2h
  • analgesia: 90 min
111
Q

What is the dosage of dex/medetomidine?

A

Dogs: 10-80microg/kg IM -alone

10-20 microg/kg IV - combination

Cats: 50-150 microg/kg IM

112
Q

What is the dosage of Romfidineromfidine

A

Horse and dog: 40-120 microg/kg IV, IM

Cat: 200-400 microgram/kg

113
Q

What is the onset of remfidineromfidine?

A

IV: 2-4min

IM: 10-20

114
Q

How long is the duration of romfidineromfidine?

A

sedation is a bit longer and causes less ataxia or recumbenxy than xylazine and detomidine

115
Q

Some drugs that have the reverse effect of alpha2-agonists

alpha2-antagonists

A

atipamezole

tolazoline

yohimbine

116
Q

What kind of drug is atipamezole, which specific drug does it reverse?

A

alpha2-adenoreceptor blocking agent

reverses the effect pf medetomidine

117
Q

what are the side effects of atipamezole?

A

it is well tolerated in dogs and cats

tachycardia

transient hypotension

hypothermia

vomiting

defecation

panting

muscle tremor

118
Q

what is the contraindication of atipamezole?

A

ketamine-medetomidine

119
Q

What is the dose of atipamezole?

A

horse: 150 microgram/kg
dogs: 5 times
cats: 2,5 times the dose of medetomidine

120
Q

What type of drugs are yohimbine and telazoline?

what drug does it have reverse effect of?

A

significant alpha1-antagonistic action

reverse effect of xylazine

121
Q

Yohombine is mainly used in combinations with another drug, which drug is it and why?

A

Fampiridine

it facilitates the release of neurotransmitters from nerve endings

122
Q

What is meant by receptoral action?

A

they facilitate or amplify the inhibitory activity of GABA

  • possibly by eliciting a structural alteration in the GABA-receptor complex, resulting in an opening of chloride ion channels
123
Q

Where are benzodiazepine receptors found?

A

located in all levels of CNS and in muscles

124
Q

What si the effect of benzodiazepines?

A

sedation and anxiolytic effect

anticonvulsive effect

muscle relaxation

hypnotic

125
Q

what is the antidote to benzodiazepine?

A

flumazenil and sarmazenil

in case of overdose of certain BDZs, dose 100 µg/ttkg IV (duration of action is to short in human)

40 µg/ttkg (horses) IV q24h, respectively

126
Q

How is the pharmocokinetics of diazepam?

  • absorption
  • binding?
  • excretion
A

oral absorption is good, IM is delayed

it binds significantly to plasma proteins

excretion: after demethylation and conjugation via the kidney

127
Q

what is the clinical use of diazepam?

A

premediacation and combination (ketmaine)

muscle relaxation

prevention and control of epilepsy

sedation

128
Q

What is the interaction and contraindication of diazepam?

A
  • paradoxical reaction
    • cat
    • greyhound
  • aminoglycosides
    • inhibition of respiration
  • before and during delivery
    • enormous high doses
  • liver diseases
    • rare hepatotoxicity esp. cats
129
Q

What is the dosage of diazepam?

A

sedation: 1-15 mg/kg PO

pre-medication: 0,2 mg/kg IV

status epilepticus: 5-10 mg/kg (dog??) IV then 2-5mg/hour IV

130
Q

How is the function of midazolam and what is the dosage?

A

shorter effect, produces less sedation than diazepam

dosage: horses 0,05-0,2 mg/kg

dogs and cats: 0,1-0,5 mg/kg IV 0,3-1 IM

131
Q

Name some anxiolytic drugs belonging to 1,4-benzodiazepines

A
  • Chlordiazepoxid (Elenium, Librium) +
  • Nitrazepam (Eunoctin) +
  • Temazepam +
  • DIAZEPAM (Seduxen, Valium) ++
  • Oxazepam ++
  • Medazepam (Rudotel) ++
  • MIDAZOLAM (Dormicum) (+AC) * +++
  • ZOLAZEPAM (Zoletil) +++
  • Alprazolam (Xanax) +++
  • Lorazepam (+AC) +++
  • Clorazepate (+AC) +++
  • Clonazepam (+AC) ++
132
Q

What is the mechanism of effects combined with baribiturates?

A

GABA-BDZ-barbiturates-receptor complex

further supposed effects: decrease in Ca2+ accumulation: inhibition in release of stimulatory transmitters stabilisation of membranes

general inhibition - but sensitivity of certain structures differs

133
Q

what are the pharmacological effects of barbiturates?

A

CNS

circulation

respiration

134
Q

what are the kinetics of barbiturates?

A

low pka - Na, K-salt

lipophylicity

lipoid/water partition

redistribution

metabolism

135
Q

What is the classification of barbiturates according to the duration of action

A

long acting - barbital, phenobarbital

middle-long action - amobarbital, butobarbital

136
Q

What is the dosage of barbiturates?

A

dose: dogs + cats PO i,5mg/kg B.I.D

tetanic horses: IV 12 mg/kg initial

6 mg/kg B.I.D to maintain

137
Q

How is the comparison between hypno-sedatives and tranquillisers?

Pharma midterm 1 (14 decks)

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