Pharma Midterm 1 Flashcards
(212 cards)
1
Q
Definition of Pharmacodynamics
A
how drug acts on body
2
Q
Definition of Pharmacokinetics
A
how drug moves in body (Principle of ADME)
(fate of the administered substance)
3
Q
Meaning of ADME
A
Absorption
Distribution
Metabolism
Excretion
4
Q
List the non specific physical interaction
A
Osmotic diuretics
Antacids
Laxatives
Chelators
5
Q
Example of Osmotic diuretics
A
Mannitol (antifreeze or ethanil glycol poisoning)
filtered in bowman’s Capsule, retains water osmotically
6
Q
Example of Antacids
A
Magnesium Hydroxide
binds to acids to elevate the pH
7
Q
Example of laxatives
A
Magnesium sulfate
Osmotically retains water in bowels
8
Q
Example of Chelators
A
EDTA (for Led Poisoning)
Deferoxamine
9
Q
Example of inhibition of enzymes
A
NSAIDs
ACE inhibitors (Angiotensin)
10
Q
Example of drug acting on Ion channel
A
Local anaesthetics (Lidocane)
11
Q
Example of drug acting on Transporters
A
Proton-pump inhibitors (Omeprazole)
Diuretics
12
Q
Example of Ligand gated ion channel and what inhibits it
A
Acetylcholine channel Receptor are inhibited by nicotinic crurare
13
Q
How may times G proteins coupled R crosses the membrane?
A
7
14
Q
Atropine is an antagonist of …
A
Acetylcholine
15
Q
PKA is activated by which receptor?
A
The Gs coupled receptor
16
Q
What happens when PKA is activated?
A
- entry of Ca
- muscle contraction (positive inotropic effect)
17
Q
Gq receptors are involved in which muscle contraction? Activated by what?
A
Smooth muscle contraction, vasoconstriction
Noradrenaline
18
Q
How do Receptor activated tyrosine kinase work?
A
Need phosphorylation to be activated, activate the AKT (Phosphokinase B)
19
Q
Example of a JAK inhibitor, and which JAK?
A
Oclacitinib, JAK
inhibits IL-4,13 and 31 (most important in allergies)
20
Q
What is EC50?
A
half maximum effective concentration
21
Q
How does an intracellular nuclear receptor works?
A
- Lipophilic receptor drugs attach to NR
- R in cytoplasm binds to HSP90 (heat shock protein)
- Ligand + complex can go in nucleus
- DNA transcription
22
Q
What is a ligand?
A
Binding + complex with receptor
23
Q
Define potency
A
power of something to influence
24
Q
How to calculate the therapeutic index?
A
LD50 / ED50
25
Example of Pharmacodynamic tolerance
Opioids, agonist continuously bin find to R --> down regulation
26
Example of Pharmacokinetic tolerance
Phenobarbital, induction of CYP450 enzymes
27
Define down regulation
Decrease in receptors on cell membrane
28
Define up regulation
Increase in receptors on cell membrane
29
True or false:
Drugs are entirely specific
False, Primary intended effects AND secondary effects
30
How can drugs be toxic?
Genetic predisposition, nonselective action, inappropriate use or administration
31
Define therapeutic window
range of doses that elicits a therapeutic response
32
A small therapeutic window means ...
The plasma level of drug must be closely monitored
33
TD50 stands for
toxic response for 50% of population
34
LD50 stands for
lethal response for 50% of population
35
ED50 stands for
therapeutically effective
36
What are the main types of classification of adverse effects of drugs?
1. "On target"
2. "Off target"
3. Production of toxic metabolites
4. Production of harmful immune response
5. Idiosyncratic responses
37
What is "On target" effect?
| how can it be adverse?
drug is binding to intended R
can be adverse if:
* inappropriate concentration
* incorrect tissues
38
What is "Off target" effect?
binds to unintended R
39
Give examples of production of toxic metabolites?
* lipid peroxidation
* Reactive oxygen species
* Depletion of GSH
40
List the 4 types of harmful immune responses
1. Imediate hypersensitivity
2. antibody dependent cytotoxic hypersensitivity
3. immune complex mediated hypersensitivity
4. delayed type hypersensitivity
41
Type 1: Imediate hypersensitivity
production of IgE
42
Type 2: antibody dependent cytotoxic hypersensitivity
drug binds to the cell, then is recognized by IgG
43
Type 3: immune complex mediated hypersensitivity
- antibodies form against soluble antigens
- complexes deposits on tissue
- can initiate response called "serum sickness"
44
Type 4: delayed type hypersensitivity
1st exposure does not produce response
repeated exposure can trigger a massive immune response
45
Idiosyncratic responses
Rare with no obvious mechanism
46
Exemples of transcellular transport:
- diffusion
- filtration
- active transport
- pinocytosis, phagocytosis
- facilitated diffusion
47
Exemple of intercellular transport:
| (btwn endothelial and epithelial cells)
filtration
48
Absorption does not occur when...
intraveanous therapy
49
Absorption determines:
the coumpound's bioavailability
50
Define the bioavailability
fraction of a drug that reaches the bloodstream
51
What can influence the bioavailability?
- Poor absorption of the GI tract
- taken with or without food
- other drugs
- the hepatic extraction
52
Give an exemple of the 3 main route of administration:
External: skin
Enteral: oral, rectal
Parenteral: IV, IM
53
What are the absorption sites after oral administration?
Stomach (weak acids, lipids), *where drugs are dissolved *
Small intestines (primary site)
54
Define distribution, and what it depends on
reversible transfer of drug from one location to another
-permeability btwn tissues
- blood flow
- ability to bind to plasma proteins
55
give the classification of distribution to various organs
brain, liver, kidney > muscle, skin > fat, bone
56
Which drugs distribute poorly to CNS
Ionized, polar drugs
57
Whicht types of drugs can cross over the placental barrier?
lipid soluble drugs
58
Define Xenobiotics:
coumpounds cannot be used as food and would be harmful if accumulated
| ( synthetic drugs, natural poisons) has no metabolic function
58
after metabolism occur what is called the new coumpound ?
metabolites
| The can be pharmocologically active (prodrugs)
59
What is the major site of biotransformation?
the Liver
60
What is the Phase 1 of biotransformation in the liver?
enzyme is catalysed, frequently a functional group that serves as active centre for sequential conjugation in phase 2
| (cytochrome P450)
60
What is the Phase 2 of biotransformation in the liver?
Conjugation reaction
| (glucuronyl transferase)
61
Cytochrome P-450
| primary location?
mechanism?
inhibition?
- liver
- drug is oxidised and oxygen is reduced to water
- competitive or not, drug - drug interaction
62
Glucuronyl transferase is not present in which species?
Cats
63
How can a drug be excreted?
Kidneys, faeces, sweat, tears, milk and lungs
64
define the first pass effect
drugs taken orally pass across membranes of GI tract into portal vein system and through liver before getting to the general circulation
65
True or False
Amount of drug in a tissue is generally related to plasma concentration
True
66
Give the 3 types of modelling
- non compartemental
- compartemental
- physiologically based
67
what is the difference between zero order of elimination and first order elimination ?
zero : constant amount is eliminated per unit of time
first: constant fraction is eliminated per unit of time
68
define one compartment model open model:
body is 1 continuous fluid with continuous loss due to excretion
69
what is the two compartemental model
the body
| has a distribution phase and elimination phase
70
how many half life is necessary to reach the steady state?
5
71
what is the steady state composed of?
average plasma concentration and range of fluctuation
| once the steady state acheived, the elimination rate is added
72
when is the loading dose used?
therapeutic concentration in plasma must be reached rapidly
73
Give 10 factors influencing the drug action
1. receptorial
2. absorption
3. distribution
4. metabolism
5. gut flora
6. health status
7. dosage
8. feeding
9. age
10. gender
74
exemple of receptorial influence on drug action
cat - morphine
75
exemple of absorption influence on drug action
horse - Ampicillin
76
exemple of distribution influence on drug action
dog - Ivermectin
77
exemple of metabolism influence on drug action
Pig - procaine
78
exemple of gut flora influence on drug action
rabbit - Penicillin
79
exemple of health status influence on drug action
Fever- decrease effect on absorption
80
define tachyphylaxis
rapid dvlpmt of drug tolerance
81
Give an exemple of idiosyncrasy
Doberman with Phenylbutazone
82
What is called a stimulant in neuropharmacology?
Psychoactive
83
What is called an inhibitor in neuropharmacology?
Psychotropic
84
list the 3 Autonomic NS medecines
Parasympatho-mimetic/lytic
sympatho-mimetic/lytic
ganglionic blockers / stimulant
85
List the somatic NS medecines
local anaesthetics
peripheral muscle relaxant
86
# In CNS
Exemple of excitatory amino acids
Glutamate
Aspartate
87
# In CNS
Exemple of inhibitory amino acids
Glycine
GABA
88
A choline ester neurotransmitter
Ach
89
A monoamines
Adrenaline
Dopamine
90
Ach acts on which R and what is its effect?
M1, closes K+, Ca2+ and Cl- channels
| depo or hyper-polarisation
91
Dopamine
precursor of NA, inhibitory effect, act on R D in basal ganglia and limbic system
92
serotonin
inhibitory effect
93
GABA
Inhibitory, acts on:
- GABAa ligand gated Cl- channel
- GABAb Gi R
94
Glycine
inhibits transmission btwn spinal interneurons and motoneurons
95
What are called CNS stimulants?
analeptics
96
exemple of analeptic acting on cortex
cocaines
ephedrines (appetite suppresant)
97
exemple of analeptic acting on medulla
doxapram (resp stimulant)
98
exemple of analeptic acting on spine
strychnine (induces reflex excitability of spinal cord)
99
True or false:
Convulsants and respiratory stimulants are used often in clinics
False, more as experimental tools
100
what drug can be used in acute resp failure?
Doxapram
101
What drug is used as an antidote for poisoning by CNS depressants
Picrotoxin
102
Exemple of central analeptics
Pentetrazol
Picrotoxin
103
Exemple of peripheral analeptics
prectamide
lobelin
104
Exemple of mixed analeptics
doxapram
105
Which drugs are methylxanthines?
caffein
theophylline
theobromine
106
in high dosage what cardiac effect has methylxanthines?
inotropic and chronotropic effects on heart
elevation of blood pressure
107
what peripheral effects has methylxanthines?
vasodilatation of coronary arteries
increase blood flow to brain, heart, muscle and kidneys
lower blood flow to GI tract
108
Side effect of caffeine?
stimulate peptic acid secretion : Peptic Ulcer
109
Clinical use of caffein?
acute heart failure
overdosing of anaesthetics
blood circulation disorder
110
What is the WP of caffein?
0 days
111
Define a seizure
group of symptoms originating from an excitement of neurones
112
why is it important to treat a seizure?
the resp. muscle are seizuring and heat can lead in brain oedema
113
Status epilepticus is ...
Generalized
114
What is the use of long term treatment of epilepsy?
a preventing treatment
115
Which guidelines are best to follow in case of an epilepsy treatment?
Consensus statement on seizure management in dogs
116
When to start a long term epilepsy treatment?
- seizure > 5min
- multiple within 3-6 months
- postictal symptoms occur for > 24 hours
- Confirmed lesions in the brain
117
For seizures what is the most important inhibitory system?
GABAa
118
Which drugs inhibits the calcium influx into the nerf for seizure treatment?
Levetiracetam
119
administration of drug for long term seizure treatment
orally
120
in which case can we discontinue seizure treatment?
- gradually
- no seizure for 2 - 3 years
121
Which is the most important drug used in seizure treatment?
Phenobarbital
122
What is the effectiveness of phenobarbital on its own?
60-90%
123
In which case is phenobarbital not recommended ?
Liver failure, intensive metabolism in liver (ROS)
124
What is the auto induction of phenobarbital?
induces cytochrom P450 enzyme system
| with time will need to elevate the dose
125
How long to reach steady state with phenobarbital?
2-3 weeks, take blood sample 1 hour before next administration to check
126
what are the side effects of phenobarbital?
* Sedation
* elevated liver enzymes
* hepatotoxicity (not in Fe)
* pancreatitis
127
how can Potassium bromide be used?
alone for mild cases
with phenobarbital
128
what are the pros of potassium bromide?
- not metabolized (so not hepatotoxic)
- long action (1 daily administration)
129
what can cause potassium bromide in cats?
bronchitis and lung oedema
130
what are the side effects of potassium bromide?
- **P**olyphagia
- **P**ruritus
- **P**araparesis
- **P**ancreatitis
131
Why would we divide potassium bromide dose in 2
to avoid emesis
132
For patients not responding to Phenobarbital or Potassium bromide, what can we combine them with?
Levetiracetam
133
is levetiracetam better in a combination or alone?
combination
134
what are the pros of Levetiracetam?
- short half life
- slightly metabolized by liver
- minimal side effects
135
what are the cons of levetiracetam?
has to be given 3 to 4 times a day
136
What is important when giving Imepitoin?
Not to miss a dosage as the half life is 2-6 hours (quick plateau)
137
which drug has a minimal changes in patients with impaired liver or kidney?
Imepitoin
138
Imepitoin has an effectiveness similar to ...
Phenobarbital
139
What is the first drug of choice while status epilepticus?
Benzodiazepines
139
What is the first drug of choice while status epilepticus?
Benzodiazepines
140
Which are the benzodiazepines used for the management of status epilepticus?
- diazepam
- Midazolam
141
Which drug can be used for the management of status epilepticus and euthanasia?
Pentobarbital
142
pros of pain
risk prevention
143
cons of pain
- catabolic state (cortisol)
- loss of appetite
- resp depression
- delayed wound healing
144
define sensitization
sense pain worse after 2 or multiple times experiencing pain
145
3 levels of pain sensitization
- peripheral sensitization
- central sensitization
- cortical reoganization
146
difference between opioids and opiates
opioids : natural and synthetics
opiates: natural (morphin)
147
True or false :
Analgesics act on nociception and nerve fibres
False, not on nerve fibres if need of amputation need to use a nerve block
148
Pharmacological effects of analgesics
Sedation, euphoria (not cats and horses), cough relief and antidiarrheal
149
What are the receptors targeted by opioids?
Which are pre-post synaptic?
Kappa, delta (presynaptic only)
Mu (pre and post-synaptic)
150
Which opioid receptor has the strongest effects?
Mu
151
Which opioid receptor agonist used are extremely safe?
Kappa agonist
152
Exemple of full agonist of opioid R
Morphine
fentanyl
153
Exemple of full antagonist of opioid R
Naloxone
| vanish side effect AND effect
154
Exemple of partial agonist of opioid R
buprenophine
155
Exemple of agonist-antagonist of opioid R
butorphanol
| antagonist: Mu R
agonist: Kappa R
156
Which drugs would be used against significant pain?
Morphine
Fentanyl
157
How can fentanyl be administered?
Topically
158
how long does it take to morphine to have its' max effect?
15-45 min
159
Side effects of opioids
- Resp drepression
- Emesis
- Bradycardia
- Obstipation
- hyperthermia
- histamine release
160
which opioid drug causes the most severe respiratory depression and bradycardia?
Fentanyl
161
Which opioid weak full agonist is unpredictable in dogs?
Tramadol
162
Which analgesic has a ceiling effect?
Buprenorphine
163
What is buprenorphine used for?
- soft tissue surgery
- pancreatitis
164
Which analgeasic is very safe?
Butorphanol
165
Exemples of other analgesics?
- ketamine
- NGF (antagonist NMDA R)
- Amantadine (antagonist NMDA R)
- Gabapentin
166
Define sedatives or tranquilizers
Induce calming by reducing irritability or excitement
167
define hypnotics
induce sleep and treatment of insomnia
168
define psychotherapeutic drugs
influence behaviour, mood and emotional reactions
169
What are the major tranquilisers (neuroleptics)
Phenothiazine derivates
Butyrophenones
170
What are the major hypnosedatives?
Alpha agonist
Anxiolytics
171
Mecanism of action of phenothiazine tranquillisers
antagonist to :
- Dopamine R
- adrenoreceptor
- muscarinic R
- H1 R
- 5-HT-R
172
pharmacological effect of phenothiazine
-sedation
- inhibition of body temparature regulation
- potentiation
- antihistamine effect
173
Administration of phenothiazine tranquilisers
buccal, rectal
174
Side effect of Phenothiazine tranquiliser
- hypotension
- irritation, allergy
- epilepsy
- **bulldogs, boxers may be oversensitive**
175
Examples of phenothiazine tranquilisers
Chlorpromazine
Propiopromazine
**Acepromazine**
Promethazine
176
Butirophenone tranquilisers mechanism of action
dopamine inhibition
NA inhibition
anticholinergic effects in CNS
177
side effect of butirophenone tranquilisers
transient salivation or panting
hypotension
178
Exemple of butyrophenones
Azaperone
179
Examples of alpha 2 agonists
- xylazine
- detomidine
- medetomidine
- dexmedetomidine
- romofidine
180
Pharmacological effects of alph agonist?
-analgesia
sedato hypnotic
vasoconstriction
GI smooth muscle relaxation
181
side effects of Xylazine
- emesis
- sweating in horses
- tympani in ruminants
182
Which specie is detomidine used for
used for Equine
183
how can detomidine be used
alone or with ketamine, thiopentone and opioids
184
medetomidine and dexmedetomidine are develloped for?
cats and dogs
185
what is romifidine frequently used with?
buthorphanol
186
What type of drug is Atipamezole and Yohimbine
Alpha 2 adenoreceptor, blocking and antagonist
187
How can diazepam be used?
Prevention and control of epilepsy
sedation
188
contraindications of diazepa
- liver diseases (cats and foals)
- paradoxical reaction ( cat, greyhound)
189
pharmacological effect of barbiturates
CNS, circulation, respiration - inhibitio
190
Example of a long lasting barbiturate and middle long lasting
long lasting: Phenobarbital
middle long lasting: amobarbital, butobarbital
191
how do local anaesthtics work?
blocks conduction in nerve fibres
192
what are the 2 chemical types of local anaesthetics
- esters (Procain)
- amides (lidocain)
193
Mechanism of action of local anaesthetics?
blocking NA+ channels
194
LA block conduction in which order
non-myelinated axons
small myelinated axons
large myelinated axons
195
give the order of the disappearance of nervous functions
- pain
- warmth
- touch
- deep pressure
- motor function
196
What influences the activity of LA
- do not work on inflammed tissue
- application with vasoconstrictor medecines increase the duration of activity and decrease the toxicity
197
Give the stages of anaesthesia
Stage 1 -disordered consciousness
stage 2 - excitement
stage 3 - surgical anesthesia
stage 4 overdose
198
Examples of injectable anaesthtics
- barbiturates
- propofol
- imidazole anaesthetics
- NMDA R antagonist (ketamin)
199
Examples of inhalation anaesthetics
- Isoflurane
- sevoflurane
- dinitrogen monoxide
- desflurane
200
Barbiturates are only applicable
IV
201
Short, ultra short acting barbiturates
Pentobarbital
Methohexital
Thiopental
202
which breed are barbiturates not used
Grey hounds (oversensitive)
203
Which anaesthetic is safe to use in liver failure patient?
Propofol
204
Opiods have to be combined with which anaesthetics?
Propofol
Imidazole anaesthetics
Steroid anaesthetics
205
How should imidazole anaesthetics be administered and why?
IV, causes severe tissue irritation
206
With which drugs can Ketamine be used
- Xylazine
- Medetomidine
- Detomidine
- Diazepam
- Acepromazin
- Butorfanol
207
What do we need for a balanced anaesthesia
combination of :
- antimuscarinic
- sedatives
- opioids
- anaeasthetics and muscle relaxants
208
combinations for light plane anaesthesia
xylazine- ketamine
Dex/Me/Detomidine - ketamine
xylazine - zoletil
medetomidine - zoletil
xylazine - butorphanol
medetomidine - butorphanol
thiopental - guaiphenesin
azaperone - metomidate (swine)
209
combinations used for neuroleptanalgesia
Etorphine - acepromazine
butorphanol - acepromazine
fentanyl - fluanisone
fentanyl - droperidol
