Introduction pharmacology Flashcards by Jassi Sangar

Drug producing 50% of maximum clinical effect?

Effective concentration (EC50)

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Drug producing 50% of maximum clinical effect in 50% of subject?

Effective dose (ED50)

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Drug dose required to produce a toxic effect in 50% of subject?

Toxic dose(TD50)

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Drug dose causing death in 50% of subject?

Letha; dose(LD50)

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dose of drug will be between ED50 and TD50?

Therapeutic window

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What does ionized (H2O soluble) does to the absorption?

Decrease absorption

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What does unionized (lipid soluble) does in the body?

Increase absorption

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Is Ka inversely proportional to pKa?

yes

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Increase in ka causes complete or partial dissociation?

complete dissociate

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Are ionized in acidic conditions

Basic drugs

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Are ioniozed in basic conditions

Acidic drugs

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HA mean?

acid unionized

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A- mean?

acid ionized

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B means

base unionized

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HB+ means

base ionized

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What are the families of receptors?

Ligand-gated ion channels
G-protein coupled receptors
Enzyme linked receptors
intracellular receptors

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Decrease in pH cause acidity to?

increase

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Increase in Ka causes acidity to?

increase

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decrease in pka causes acid to?

increase

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Example of ligand-gated ion channels are?

cholinergic nicotinic receptor

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ligand-gated ion channel causes:

cell membrane
neurotransmission
muscle contraction

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In G-protein coupled receptor, GDP switches to?

GTP

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When the drug/ligand binds to GPCR what does it triggers?

phosphorylation

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WHat subunit binds to gtp to cause cellular response?

alpha

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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

ganglia and CNS

This nicotinic receptor has role in alzheimer's

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

Introduction pharmacology Flashcards

(194 cards)