Introduction pharmacology Flashcards
Drug producing 50% of maximum clinical effect?
Effective concentration (EC50)
Drug producing 50% of maximum clinical effect in 50% of subject?
Effective dose (ED50)
Drug dose required to produce a toxic effect in 50% of subject?
Toxic dose(TD50)
Drug dose causing death in 50% of subject?
Letha; dose(LD50)
dose of drug will be between ED50 and TD50?
Therapeutic window
What does ionized (H2O soluble) does to the absorption?
Decrease absorption
What does unionized (lipid soluble) does in the body?
Increase absorption
Is Ka inversely proportional to pKa?
yes
Increase in ka causes complete or partial dissociation?
complete dissociate
Are ionized in acidic conditions
Basic drugs
Are ioniozed in basic conditions
Acidic drugs
HA mean?
acid unionized
A- mean?
acid ionized
B means
base unionized
HB+ means
base ionized
What are the families of receptors?
Ligand-gated ion channels
G-protein coupled receptors
Enzyme linked receptors
intracellular receptors
Decrease in pH cause acidity to?
increase
Increase in Ka causes acidity to?
increase
decrease in pka causes acid to?
increase
Example of ligand-gated ion channels are?
cholinergic nicotinic receptor
ligand-gated ion channel causes:
cell membrane
neurotransmission
muscle contraction
In G-protein coupled receptor, GDP switches to?
GTP
When the drug/ligand binds to GPCR what does it triggers?
phosphorylation
WHat subunit binds to gtp to cause cellular response?
alpha
WHat is the example of GPCR
alpha adrenergic receptors
Example of enzyme-linked receptor?
insulin receptor
Which enzyme is involved in enzyme-linked receptor?
tyrosine kinase
once tyrosine kinase is ______ it triggers response
phosphorylated
Example of intracellular receptors:
steroid
thyroid
nuclear receptor
What does intracellular receptors do?
targets DNA to cause gene modification
Ocuurs when one signalling molecule produces changes in thousands of proteins
Signal amplification
drug binds to receptor?
Affinity
drug produces clinical response
potency
Increase in potency cause __ in drug concentration
decrease
drug to produce response during interaction with receptor
efficacy
drug-receptor complex to prduce maximal clinical effect
intrinsic activity
ability of 1 drug molecule to interact with 1 receptor to produce response
intrinsic efficacy
What are the 4 types of drug interaction?
Synergism
Addition
potentiation
antagonism
This drug interaction means combination drug has greater effect than individual drugs (Effect Ab» Effect A + effect of B)
Synergism
This drug interaction means one drug increases the effect (or protects the) of another drug.
potentiation
Example. of potentiation
Levodopa+carbidopa and amoxicillin+clavulinic acid
This drug-receptor interactions activates the receptor?
Agonist
This drug-receptor interactions inhibits/attenuates agonist effect?
antagonist
produces Full effect
Full agonist
does not produce 100% activation
partial agonist
produces opposite effects of the agonist and effect is below the baseline
inverse agonist
Example of inverse agonist
anti-histamines
drugs binds to agonistis receptor site, can be overcome by increase in agonist
competitive inhibition
drug binds to allosteric site
non-competitive inhibition
Reversible antagonist can be reversed with increase in?
substrate
Produces lower effect after prolong use of drug same dose
Downregualtion
Example of downregulations are”
opoids
alcohol
nicotine
Produces higher effect after prolong use with same dose?
supersensitization
example of supersensitization
antipsycotic drugs
dyskinesia
send signals from BRAIN to ORGANS
Efferent
send signals from ORGANs to BRAIN
Afferent
This ANS nerve has long preganglionic nerve and short postganglionic nerve?
Parasympathetic
In parasympathetic system postganglionic nerve Ach binds to which receptor
Muscarinic receptor
This system also known as rest and digest
Parasympathetic
This ANS system responses to emergency situation
sympathetci
In this ANS system has NE at posganglionic nerve and binds to :
sympathetic and binds to alpha and beta
Is the origin of sympatheic nerve?
thoracolumbar
origin of parasympathetic nerve?
craniumsacral
This is also known as fear, fight and flight?
sympathetic
What are the sympathetic effects on Heart?
Increase cardiac outputs (increase in BP and HR). increase conductivity
What are the sympathetic effects on BV?
Vasoconstriction and vasodilation
Vasoconstrictions happens in which blood vessel?
skin and mucus membrane
vasodilation happens in which BV?
coronary and skeletal muscle
What are the sympathetic effects on Respiratory system?
bronchodilation
What are the sympathetic effects on GIT?
constipation and urinary retention (relaxes the sphincter)
What are the sympathetic effects on male sex organ?
ejaculation
What are the sympathetic effects on female sex organ?
relaxation of uterus
What are the sympathetic effects on Eyes?
mydriasis
far accomodation (ciliary muscles relaxes)
closes canal of schlemm (increase in IOP-glaucome)
What are the sympathetic effects on Exocrine glands?
viscous secretions causes dry mouth
What are the sympathetic effects on metabolism?
glycogenolysis
lipolysis
gluconeogenesis
This system control the radial muscle?
sympathetic
Parasympathetic control which muscle in the eyes?
circular muscle
Sympathetic receptors also known as:
Adrenergic receptors
Example of adrenergic receptors
alpha and beta
parasympathetic receptors AKA:
cholinergic receptors
M1 (muscarinis 1 receptors) is responsible for:
cognitive
M2:
smoth muscles
Nm is
motor end plate of muscles
Nn
ganglia and CNS
This nicotinic receptor has role in alzheimer’s
Nn
What si the effect of vagal nerve on CNS and heart?
slows down the heart rate (bradycardia)
What is the orgin of sweat gland?
thoraculumbar
sweat gland has this receptor at posganglia
Ach on muscarinic
What are the 3ways to stop sympathetic effects?
MAO
COMT
Reuptake of NE
Way to stop PS effect?
Acetylcholinesterase - inhibits Ach
is an autoimmune disease where nicotinic muscular (NM) receptor is damaged
Myasthenia gravis
Myasthenia gravis causes:
weak muscle tone
SE of Myasthenia gravis are:
drooping eyelid
trouble talking
trouble walking
What are the examples of direct acting cholinergic agonsit:
Choline esters
cholinomimmetic alkaloids
Example fo choline esters:
Methacholine
Bethanocholine
Carbachol
MOA of Choline esters:
Ach mimmetics
this choline ester is used for post-ocular surgery
carbachol
a choline ester bethanecol is used for
urinary retention
a choline ester methacholine us used for
test for asthma
example of direct acting cholinomimmetic alkaloids
pilocarpine and cevemeline
MOA of direct actin cholinomimmetic alkaloids in mouth and eyes is:
induces saliva secretion
decrease IOP
Pilocarpine is used for
dry mouth and glaucoma
Example of indirect action acetylcholinesterase antagonist are:
reversible and irreversible
Example of irreversible cholinesterase inhibitors are:
organophosphate compounds
irreversible cholinesterase inhibitors causes:
Bronchospasm
salivation
lacrimation
convulsions
Reversible cholinesterase inhibitors are belongs to which family:
Stigmine family
is an antidote for atropine toxicity and passes BBB (tertiary amine)
physostigmine
this drug is used for diagnosis(edrophonium) and txt for myasthenia gravis
neostigmine (prostigmine)
Antidote of curare poisoning
neostigmine (prostigmine)
used for post-operative urinary retention and paralytic ileus
neostigmine (prostigmine)
Is used for txt of myasthenia gravis
pyrodostigmine and ambenonium
used for diagnosis of myasthenia gravis and is short acting drug (5 minutes)
edrophonium
These drugs are used alzheimer’s disease
Rivastigmine and donepezil
This drug is the father of parasympatholytic drugs
atropine
Atropine is an
anticholinergic and muscarinic blocker
7 common SE of anticholinergic drugs (atropine)
Tachycardia Blurred vision photo[hobia dry mouth urinary retention constipation hallucination excitation fever (no sweating)
atropine is used for:
mydriasis
dry secretions
organophosphate toxicity
antispasmodic
This atropine like medication is used as atropine substitute for mydriasis and is short duration
homotropine and tropicamide
Anti-parkinsons drugs are:
benzotropine and trihexphenidyl
used for bronchial asthma and COPD
Spiriva and atrovent SE: dry mouth
Atropine like meds that does not pass BBB:
Toviaz
Solifenacin
oxybutynin
Example of direct acting sympathomimemtic agents:
epinephrine (alpha, beta) NE (a) Isoprenaline (b) phenylprenaline (a1) salbutamol(b2) dobutamine(b1)
Act by increasing the release of NE from vesicles
indirect acting sympathomimetic agents
Example of indirect acting sympathomimetic agents
tyramine
amphetamine
example of mixed acting sympathomimetic agents
ephedrine
Example of alpha 1 agonists are:
Phenylephrine xylometazoline pseudoephedrine ephedrine methoxamine
alpha 1 agonists are used for:
congestion
pupil dilation
hypotention
examples of alpha 2 agonists are:
methyldopa and clonidine
alpha 2 is used for:
hypertension
SE of clonidine
rebound hypertension
Is weak antihypertensive agent
clonidine
B1 drugs are:
dobutamine
B2 drugs are:
SABA : salbutamol, terbutaline, isoproterenol
LABA: salmeterol , formoterol
b3 drugs are:
mirabegron
b1 and b2 drugs are:
isopreternol
b1 drugs are used for:
heart failure
bradycardia
heart block
b2 drugs are used for:
asthma
copd
respiratory disease
prevents premature labor
b3 drugs are used for:
overactive bladder
b1 and b2 drugs are used for
bronchial asthma (only isoprenaline)
Amphetamine like drugs are:
Amphetamine(dextroamphetamine) methamphetamine methylphenidate tyramine ephedrine
amphetamine like drugs are used for:
narcoplesy
ADD
ADHD
MOA of amphetamine like drugs
increase release of catecholamines
SE of amphetamine like drugs
Anorexia stomach upset restlessness increase HR and BP elevated adrenereceptros activation inhibits physical growth
What are the 3 classification’s of sympatholytic drugs:
ARB (adrenergic receptor blocker)
ANB(adreergic neuron blocker)
CAD(centrally acting drugs)- clonidine and alpha methyl dopa
Drugs that inhibts the NE relase
Guanithidine
Drugs that inhibit NE STORAGE
reserpine
drugs that inhibit NE synthesis
alpha methyl dopa
5 uses of a1 blockers:
Prostate enlargment Peripheral vascular disease Phaechromycytoma Hypertension Erect dysfunction
Alpha blockers belong to which family:
Zocine family
Common 5 SE of a1 blockers as vasodilators:
Reflex tachycardia postural hypotension headache flushing congested nose
example of a2 blocker
yohimbine
non-selevtive b blockers are:
Nadolol sotalol timolol propranolol pindolol
b blockers are used for:
Hypertenions arrythmia congestive heart failure glucoma angina (avoid non-selectiv)
What are the types of Aneshtesia?
Local and General Anesthesia
Is the reversible state of CNS that eliminates perception and response to external stimuli.
Anesthesia
Stages of Anesthesia:
induction
Maintenance
Recovery
General anesthesia act by?
increasing GABA receptor
decrease NMDA or aspartate glutamate
GA act on?
inhibiting Reticular activating system (RAS)
What are the 4 depts of Anesthesia?
Analgesia
Excitement
Surgical anesthesia
Medullary paralysis
What are the two types of GA?
Inhaled and IV
This type of GA is used for maintenance stage of anesthesia?
Inhaled GA
Give 2 classes of Inhaled GA:
Nitrous oxide
Fluranes
Give 4 classes of IV GA:
Propofol
ketamine
thiopental (barbiturate)
midazolam (benzo)
What are the 5 conditions to be worried about if administering Inhaled GA?
CVS Respiratory Liver CNS Malignant hyperthermia
this is the oldest member of flurane?
Halothane
This is the best direct muscle relaxant but is irritant to the lungs?
Isoflurane
This flurane has no odour and has less side effect compared to other members of flurane family?
Sevoflurane
What causes malignant hyperthermia?
Halothane
What causes neurolyptic malignant syndrome (NMS)
Antipsycotic drugs
This anesthethic blocks the sodium channels.
Local anesthetic
What are the 2 classes of Local anesthetics?
Esters
Amide
Examples of Ester LA:
Benzocaine
Cocaine
Procaine
Tetracaine
Examples of amides LA:
Lidocaine
Bupivacaine
Ropivacaine
This amide causes arrythmis, bradycardia and it is the weak LA.
Lidocaine
This is the strong LA:
Bupivacaine
What are the pre-anesthetic medications?
BASAAO Benzodiazepines Anticholinergic Skeletal muscle relaxant Antihistamine Antiemetic Opoid analgesics
This anticholinergic drug avoids bradycardia
atropine
This preanesthetic med calms the pt.
Benzodiazepines (diazepam)
What are the 3 different classes of drugs Na channel blockers?
Class I antiarrythmia
Anti-epileptic (carbamazepine and phenytoin)
LA
THis is AKA Laughing gas
Nitrous oxide
Nitrous oxide is commonly known as Laughing gas and as well _____.
incomplete anaesthesia
80% N2O should be mixed with how much of O2 if giving as LA.
20%
This IV GA is NMDA antagonist
ketamine
Ketamine produces state of?
Dissociative anesthesia
This IV GA drug cannot be used in pregnancy
Ketamine
This peripherally acting drugs inhibits the synthesis of Ach
hemicholinium
This peripherally acting drugs stops the release of Ach
botulinum toxin
This competitive nerumuscular blocker (NMB) release histamine and produces flaccid paralysis as well
Curare
This is the antidote of curare
neostigmine
This depolarizing NMB produces spastic paralysis
Succinylchloride
Succinylchloride is metabolized by
pseudocholinesterase
What are the centrally acting drugs?
Baclofen
Tizanidine (Sirdalol)
Flexinire
Methicarbamol
This type of skeletal muscle relaxant decreases Ca release from sarcoplasmic reticulum leading to inhibiton of muscle contraction
Direct -acting muscle relaxant
This is the DOC for malignant hyperthermia and it is direct acting muscle relaxant.
Dantrolene