Year 1 Drugs List (Medicine)

8/16/2019 Year 1 Drugs List (Medicine)

1/33

Drugs Type of

drugsName and

pharmacokineticAdministration or

clinical useMechanism of action

Side eect orelimination

Nicotinicreceptor

Neuronaltype

Agonist: nicotine

activates bothsympathetic andparasympatheticnervous system

autonomicconfusion

Antagonist:hexamethonium

loss of sympatheticand parasympatheticreexes! especiallycardiac tissue

Muscle

type

Agonist:suxamethonium"depolari#ingNeuromuscularblocking drugs$

to induce muscleparalysis for surgery"muscle relaxation$

suxamethonium brokendo%n by plasmacholinesterase toinactivate metabolites

Antagonist:atracurium"NondepolarisingNMD$

competitive antagonistaction! action reversedby anticholinesteraseseg:neostigmine

Muscari

nicreceptor

Muscarinicagonist &ilocarpine

treatment of glaucoma

• causes ciliarymuscle tocontract! openingthe trabecularmesh%ork'

• (t facilitates the

rate that a)ueoushumour leaves theeye to decreaseintaocularpressure

treatment ofS*ogren+s syndrome


2/33

Drugs Type of drugsName and

pharmacokineticAdministration or clinical

useMechanism of

actionSide eect orelimination

Muscarinicreceptor

Muscarinicantagonist

atropine ortropicamide

• dilate the pupil

and paralyseaccomodation toenable eyeexamination

• premedication tosupressrespiratory andsalivary secretion

competitivelyantagonise the

eects of Ach atmuscarinicreceptors

• blurred

vision• mydriasis

• pupildilatation

• urinaryretentionconfusion

• constipation

• feveripratropium ortiotropium

dilatation of bronchialsmooth muscleeg: asthma and ,-&D

atropine. short half.life"/0h$. anticholinergic

adverse eect. hepaticmetabolism

Administered (1

treatment of sinusbradycardia eg: after M(

Muscarinicreceptor

muscarinicantagonist

hyoscine • relax 2( smoothmuscle for motionsickness

• to facilitateendoscopy

• antispasmodic inirritable bo%eldisease

• premedication tosuppressrespiratory andsalivary secretion

competitivelyantagonise the

eects of Ach atmuscarinicreceptors


3/33

piren#ipineinhibit gastric secretion

Drugs Type of

drugsName and




Sympathetic

NervousSystem

Adrenergicagonist

&henylephrine 3or nasal decongestion

• Acts on 45 receptor

• 1ascular smoothmuscle"vasoconstriction$

,lonidine3or hypertension andmigraine Acts on 46 receptor

Dobutamine3or cardiogenic shock"reduced myocardialcontractility follo%ingM($


• 8eart "increaseheart rate andforce$

Salbutamol 3or asthma andpremature labour

• Acts on 76 receptor• 9ronchial smooth

muscle"bronchodilatation$

pinephrine • (ncreaseduration ofaction of localanesthetic

• ,ardiac arrest


4/33

• Shock"vasodilatation$andbronchospasmin response toan allergen

Drugs Type of

drugsName and


clinical useMechanism of action Side eect or elimination

Sympathetic

NervousSystem

Adrenergic

antagonist

&henoxyben#ami

ne

3or phaechromocytoma"causes irreversible

blockade ofadrenoreceptor$

• Acts on 45 and 46 receptor

• 1asodilatation

• 3atigue

• 9ronchoconstriction

• Sexual dysfunction• Arrhythmias

• 9radycardia

• 8ypotension

Doxa#osin

• 3or hypertension

• 9enign prostatichypertrophy"inhibithypertrophy$


• 1asodilatation

Non.selective 7.blocker:

5' &ropranolol

6' Timolol

• Treating

myocardialinfarction

• Treatinghyperthyroidism

• Treatingglaucoma"reduce secretionof a)ueoushumor$

• Acts on 75 and 76

receptor• 8eart "decrease

heart rate and force$

• 9ronchoconstriction


5/33

• Treating angina"propranolol$

,ardioselective 7antagonist:

5' 9isoprolol6' Atenolol0' Metoprolol

• Anti.

hypertensivedrugs ",- andrenin secretionreduced$

• Treating angina"bisoprolol$


• 9ronchial smoothmuscle"bronchodilatation$

Drugs Type of

drugsName and




Anti.clotting;

antithrombotic drugs

Anticoagulants 5' 8eparin

6'


6/33

=arfarin• 8alf.life

"5.BC hours$• Dose is highly

variable• @apidly and

almost totallyabsorbed from2(T

•


7/33

Direct thrombin"factor ((a$ inhibitors

5' lepirudin6' Dabigatran

• @apid onset ofaction

• Does notre)uiremonitoring

•


8/33

9loodpressurelo%ering

drugs

A,(nhibitors

5' ,aptopril

• =ell absorbedorally

• 8alf.life 6h

•

&artlymetaboli#ed andpartly excretedunchangedrenally

6' napril

• =ell absorbedorally

• &ro.drug'Metaboli#ed to

enalaprilat"longer half.life$

• T%ice dailyadministration

0'


9/33

Angiotensin@eceptor9lockers

"A@9$


10/33

7 adrenoreceptorantagonists "7 blockers$

5' Non selective

• &ropranolol. short half life

"0.h$

6' Selective"half.life .Bh$• Metoprolol

• Atenolol

• Acebutolol

Non.selective. undergoes Frst.pass hepaticmetabolism "poororal bioavailability$

. lipid soluble"crosses 999$. not commonlyused formanagement ofhypertension;heartfailure

Selective. %ater soluble"does not cross999$. CE absorbedorally. eliminateunchanged in urine. accumulates inrenal failure. use forhypertension and inchronic congestiveheart failure %ithA,(s. use in acute heartfailure

• K 8@ . K rateofspontaneousdepolari#ation

! slo%conduction inatria and A1node

• K myocardialcontractility

• (nhibit @AAS

• Kperipheralresistance

• 9ronchospasm

• 8eart failure"due to Oveinotropiceects$

• 9radyarrhythmias! coldextremities!fatigue!sleepiness!

vivid dreams• Mask

hypoglycaemia symptoms

• 9eta.blocker%ithdra%alsyndrome "Lsensitivity tocatecholamines O %orseningangina$

Drugs Type of

drugsName and


clinical useMechanism of action Side eect or elimination

9loodpressurelo%ering

Diuretics Thia#ide diuretics• hydrochlorothia

#ide

,linical use:• mild to

moderate

• lectrolyteimbalance. hypokalemia


11/33

drugs

hypertension

• K 9& by depletingbody sodiumstores. K&1@ "sodiumincreaseperipheralresistance byincreasing vesselstiness andneural reactivity$

• @educe bloodvolume. K ,-

. hyperkalemia

. hypomagnesemia

. hyponatremia

• 8yperuricemia


12/33

Drugs

Type of

drugs

Name and

pharmacokinetic

Administration or

clinical use Mechanism of action Side eect or elimination9lood

pressurelo%ering

drugs

o Metaboli#ed inliver by,H&0AI

6' 9en#othiapine. Diltia#em

0' &henylalkylami

ne. 1erapamilNitrates @apidly metaboli#ed

by liver

• 2TN not givenorally

• (SDNmetaboli#ed tomore activemetabolite"longer

duration ofaction$

*nitrate to$erance canbe overcome by%& nitrate gap ('h#& Administerinreuent$y

• 2lyceryltrinitrate "2TN$O sublingual!transdermalpatch

• (sosorbidemono ordinitrate Osublingual! oral

• Nitroprusside O(1

• Amyl nitrite"inhalant$

,linical use:. stable and unstableangina. acute heart failure

• Nitric oxide donor'Lc2M& leads tosmooth musclerelaxation

• &eripheralvasodilation"venodilation RRarterial dilation$

• Dilate coronary

arteries. L blood supplyto heart. redistribution ofcoronary bloodo% to ischemicmyocardium

• &ostural

hypotension

• Tachycardia

• Throbbing

headache

• 3lushing


13/33

& give sma$$estefective dose

and chronic heartfailure

1asodilators

Minoxidil

• C E oralbioavailability

• 8alf.life Ih

1ery ecacious orallyactive arteriolardilator

. -pening of G Q channel

in smooth musclemembranes by minoxidilsulfate. Associated %ith reexsympathetic stimulationand sodium and uidretention "use incombination %ith ablocker and loopdiuretics$

• @eex sympathetic

stimulation:

tachycardia!

palpitations!

angina

• Ankle s%elling

• 8ypertrichosis

Drugs Type of

drugs

Name and

pharmacokinetic

Administration or

clinical use

Mechanism of action Side eect or elimination

9lood

pressure

lo%ering

drugs

1asodilator

s

8ydrala#ine

• =ell absorbed

arteriolar dilator

•


14/33

(notropic

agents

• Digoxin. good oral

absorption. renal RR

hepatic

elimination. half.life 0h. narro%

therapeutic

index

ar arrhythmias

• ,hronic atrial

Fbrillation

• 8eart failure

3actors aecting

Dixogin toxicity:

. hypokalemia

. hypercalcemia

. hypomagnesemia

. renal impairment

. hypoxemia

. hypothyroidism

Treatment of dixogin

toxicity:

. %ithhold drug

. G Q supplementation

if hypokalemic

vagal tone "K

rate and

conduction

velocity in sinus

and A1 node$• (notropic O inhibit

Na;G AT&ase

pump! L

intracellular ,a6Q

• Supraventricular

and ventricular

arrhythmias

Non cardiac

•

Nausea! vomiting!constipation

• ,onfusion! vertigo!

hallucination!

disorientation

• 1isual disturbance

"yello% halos

around light$

Drugs Type of

drugs

Name and

pharmacokinetic

Administration or

clinical use

Mechanism of action Side eect or elimination

. atropine for sinus

bradycardia

. ventriculararrythymias:

&henytoin! lidocaine9ipyridine

5' Milrinone6' (namrinone

. Available only in

parenteral forms

Jsed (1 only for acute

cardiac failure or

severe exacerbation

of chronic heart

failure

(nhibit

phosphodiesterase

iso#yme 0 "&D.0$

%hich LcAM&

• Nausea;vomiting

• Arrhythmias

• Thrombocytopenia

•


15/33

. 5C.ICE excreted in

urine

. 8alf.life 0.h

changes

75 agonists

5' Dobutamine. rapid onset. steady state in

5C mins. half life 6mins

6' Dopamine

,linical uses:

• Acute short

term use• To treat acute

cardiac failure

in post M(

• Jse in

cardiogenic

shock

Stimulate cardiac 75receptors "Qve

inotropic$

Diuretics

&otassium

"G Q$ losing


16/33

n excretion of NaQ!

G Q! 86-

• 1asodilator

eect

• rectile

impotence

&otassium "G Q$

sparing

Aldosterone

antagonists

5' Spironolactone. half.life 5C mins

6' plerenone. half.life .5h

Steroid structure

&ro.drug O action via

activate metabolite

canrenone

(mproves survival

in chronic heart

failure

• ,ompetitive

antagonist of

aldosterone

• (nhibits

aldosterone.

induced

production of Na

transport

proteins at D,T

U ,T• @esults in NaQ

and 86- loss! G Q

retention

• 2ynecomastia!

menstrual

disturbances!

reduced libido!

testicular

atrophy• 8yperkalaemia!

2( disturbance

Aldosterone

independent

5' Amiloride6' Triamterene

8alf.life h

&oor oral

absorption• Aldosterone.

independent

inhibition of

D,T;,D sodium

transport

• @esults in NaQ

and 86- loss! G Q

retention

• 8yperkalaemia

• 8yponatremia

• 2( disturbance

V5;76

adrenoreceptor

agonist

(soproterenol

"isoprenaline$

. short half.life

"minutes$

• Administere

d (1

• 3irst pass

metabolism

Sympathomimetic

adverse eects

. tachycardia

. arrhythmias

Drugs Type of drugs Name and

pharmacokinetic

Administration or

clinical use

Mechanism of action Side eect or

elimination,lass (a


17/33


18/33


pharmacokinetic

Administration or

clinical use


elimination,lass (((

. G channel

blocker

. inhibit &hase (((

repolarisation

5' Amiodarone. long half.life

5C.5CC days. hepatic

metabolism6' Sotalol0' DronaderoneI' (butilide

. ective for

ventricular and

supraventricular

arrhythmias

. Frst line for

treatment of

ventricular

Fbrillation

. improves survival

in patients %ith

recurrent 1T

• &rolongs A&

duration and

refractory period

•


19/33

depolarisation . diltia#em

0' &henylalkylamine. verapamil

&redominantly cardiac

eects ".ve intrope and

chronotrope!

antiarrhythmic$

-thers ",lass 1$ 5' ,ardiac

glycosides

"Digoxin$. vagolytic

(ndication:

. supraventricular

arrhythmias

. chronic A3

. heart failure

. Antiarrhythmic:

vagotonic eect reduce

rate and conduction

velocity in sinus and

A1 nodes

. (notropic

"L intracellular ,a6Q$


pharmacokinetic

Administration or

clinical use


elimination

6' Adenosine. antipurinergic

Short half.life

Administered (1

(ndication:

. diagnosis and

termination of

supraventricular

arrhythmias

adenosine 45 and 46

agonist

. cardiac 45 receptors ".

ve inotropic and

chronotropic$

. vascular 46 receptors

"vasodilatation$

• ,hest pain!

ushing!

bronchospasm

"avoid in

asthma$!

headache• A1 block "avoid

in 6nd;0rd degree

heart block$0' Magnesium

sulphate


20/33


pharmacokinetic

Administration or clinical

use


elimination

Type 5

Diabetes

@apid acting 5' (nsulin aspart6' (nsulin lispro0' (nsulin

glulisine

Soluble insulin %hich

do not readily form

dimers;hexamers

S, "routine$

(1 administration

"emergency$

S, in*ection faster onset

and shorter duration of

action than soluble

insulin

(n*ected "S,$ from

5min before to

immediately follo%ing

the start of a meal

Administered to mimic

the prandial

"mealtime$ release of

insulin

Short acting 5' Soluble insulin"regular

insulin$

Native or regular

insulin associate as

hexamers in neutral

p8' This aggregation

slo%s absorption

2iven (1! (M and S,

S, O rapid onset "0C.

Cmins$

. peak bet%een 6.Ih

(1 O very short half.life

(n*ected "S,$ from 0C.

Imin before start of a

meal

Jse for diabetic

emergencies

eg: diabetic ketoacidosis(ntermediate

acting

5' (sophane

insulin "N&8

insulin$

9roken do%n slo%ly

subcutaneously and

absorbed at slo% rate'

. onset of action 5.6h!

max eect I.56h

Suspension of native

insulin! complexed

%ith #inc and

positively charged

polypeptide protamine


21/33

-nly be given S, "never

(1$

"solution is cloudy! in

contrast %ith other

insulins$


pharmacokinetic

Administration or

clinical use


elimination

Type 5

diabetes

Jsed for basal control:

. once daily at bedtime

T%ice a day in

combination %ith short

acting insulin


22/33

Type 6

diabetes

-ral

hypoglycaemic

agents

channel

• K hepatic

glucose

production• L peripheral

insulin

sensitivity

• hyperinsuline

mia

9iguanides

5' Metformin

. oral availability of

C.CE

. not bound to

plasma protein! half.

life 0h

,an suppress appetite

and causes less %eight

gain than

sulphonylureas "useful

in over%eight people

%ith diabetes$

• K hepatic

glucose output• Slo%s intestinal

absorption of

sugars

• (mproves

peripheral

glucose uptake

and utilisation


23/33

Type 6

Diabetes

-ral

hypoglycaemic

agents

resistance in

liver and muscle

• nhances

uptake of 3A

and glucose

• Suppress

glucose

production in

liver4.glucosidase

inhibitors

5' Acarbose

. 8as no eect on

insulin secretion;its

tissue action

.


24/33

Type 6

Diabetes

-ral

hypoglycaemic

agents

%ith insulin$ %ith

improved stability and

solubility

promotes satiety

(ncretins

5' 2


25/33

level

Drug Name/Ty

pe

Administration Caution Pharmacokinetics Adverse Eect

8ypothyroidism


26/33

ne "T0$ (1

• 3or

myxoede

ma coma

.x more potent

than TI

.8alf.life: .B hrs

.Maximum eect

in 6I hours

"plasma protein

bound$

.Dose: 5C.6C

microgram

bd;tds

!yperthyroidism Drugs

Drug Type/Name "echanism o#

Action

Clinical $se Pharmacokinetics Adverse Eect

(odine

Jptake

(nhibitors

Anions

.perchlorate

.pertechnetate

.thiocynate

,ompetes %ith iodide

for follicular cell

uptake .R decreased

iodide for thyroxine

synthesis


27/33

(nhibitors

of

-rganiFcati

on;(odinatio

n and

8ormone

@elease

Thionamides; Thioami

des;

Thioamines; Thioureyl

enes

.methima#ole "MMl$

.carbima#ole ",Ml$

.propylthiouracil

"&TJ$

,ompetes %ith

thyroglobulin tyrosine

for iodination

>&TJ

.also deiodinase.5.

inhibitor:

inhibits peripheral

conversion of TI .R T0

at high doses

.preferred in thyroid

storm

2raves Disease

.MM(! ,M(! &TJ

ither

.add in thyroxine

5CCmicrogram;day

"block U replace$

.reduce dose to

5C;6Cmg od

"tailored dose$

Duration of

therapy: 5.6 yrs

gives /CE long.

term remission

.mechanismunkno%n:

\immunomodulator

y]

,M(

.half.life: I. hours

.accumulates in

thyroid

.metaboli#ed in

thyroid and

else%here

.cross placenta!

breast milk

.@enal excretion

>MM(

.active metabolite

of ,M(

&TJ

.half.life: 6 hours

.plasma.protein

bound

.less crossing to

placenta and breast

milk: preferred in

pregnancy

Ma*or

.neutropenia

.agranulocytosis

.aplastic anemia

.

thrombocytopeni

a

.hepatitis

.drug induced

vasculitis

Minor

.rash! itch

.arthralgia!

arthritis

.headache

.nausea! gastritis

.hair loss

.abnormal taste

@adioactive (odine "

I 131

¿

.best treatment for:Nodular

thyrotoxicosis

"TM2! solitary toxic

adenoma$

.thyroid

storm;counteract

.half.life: B days

.eect %ithin: 5.

6mth


28/33

proceeding

hyperthyroidism bI

thyroidectomy

.single oral dose

cures RBCE ofpatients

>absolute

contraindication:

pregnancy;breast.

feeding

"x conceive for

months$

>best avoided inchildren

(odide;(odine

.-ral preparation:


29/33

%ho already

have

hyperthyroidism

.%; amiodarone

.R destructive

throiditis.radiographic

contrast agents

.supplementation

in diet

• ^od.

9asedo%

eect

"autoimmu

ne!

nodular

thyroid

disease$

.allergic reaction

(nhibitors

of

&eripheral

Thyroid

8ormoneMetabolism

.b.blocker

.ipodate

.glucocorticoid


30/33

Drug Name/Type Administration Clinical $se "echanism o#

Actions

%ide

Eect/Characteris

tic9ronchodilati

on

β2

Agonist"5st line$

Short.Acting

.Salbutamol

.Nebuliser

.Aerosol inhalation

.&o%der inhalation

Acute asthma

.-nset: .

0Cmins.@elief: I.

hours

.tremor

.tachycardia

.cardiacdysrhythmia

side.eect

minimise %hen

administered

through inhalation

vs' via systemic

circulation

MuscarinicAntagonist

"6nd line$

.ipratropium• -nset:

0C.C

mins• 8alf.delayed phase:

inammatory

response

"inammation!

mucous!

bronchospasm$

>immediate phase:

bronchospasm

Side ects:

.inhaled: dry mouth

U 2( upset

.nebulised:

mydriasis "pupil

.tiotropium

• 8alf.


31/33

dilation$

Theophylline"6nd;0rd line$

.oral "sustainedrelease$

.9ronchodilatio

n

.(nhibit

delayed phase

.inhibitsphosphodiesteras

e

>&hosphodiestera

se converts cAM&

.R AM&! inhibiting

the path%ay that

decreases systolic

calcium

.drug.druginteractions %ith

,H&0A inhibitors

.narro% therapeutic

index

.supratherapeutic

levels:

• 2( eects

• 8eadache

• (rritability

• (nsomnia.higher

supratherapeutic

levels:

• ,NS: sei#ure!

toxic

encephalopat

hy

• ,1: cardiac

arrhythmia!

death


32/33

.lipoxygenase inhibitor

.#ileuton

.oral

• CE plasma

protein

bound

• All

extensively

metabolised

.Asthma

prophylaxis

.Decrease

eects of

Aspirin

sensitiveasthma

"intrinsic

asthma$

(nhibits .

lipoxygenase

>.lipoxygenase

transforms

arachidonic acidinto leukotrienes

.All are %ell.

tolerated %ith fe%

adverse eects

• 8eadache

• 2(

disturbances

• Xileuton:

8epatotoxicit

y

•


33/33

phospholipid into

arachidonic acid

>,yclooxygenase

converts

arachidonic acidinto

prostaglandinsAnti.(g

.omali#umab

.prevents (g!

prevents release

of chemical

mediators by

mast cells

Date post:	06-Jul-2018
Category:	Documents
Upload:	anonymous-iwwt90vy
View:	215 times
Download:	0 times

Year 1 Drugs List (Medicine)

Documents