Pharmacokinetics & Drug Interactions
Pharmacokinetics & Drug Interactions
FlCADEMIC PANELIST
general consideration before admin. pharmacokinetics interactions pharmacodynamics interaction after admin. (inside body) permeation of drugs across cell membrane
mechanism
Drug interaction
absorption
factor affecting routes of drug factors affecting oral absorption patterns distri bution binding to plasma protein
Pharmacokinetics
General
Pharmacokinetics Principle
Receptors
bioavailability
General.mma
- 24/5/2011
- Mindiet
Acetycholine Choline
ZAGAZIG ACADEMIC PANELIST
Other choline
Methacholine
Bethanechol
Cholinomimetic
Alkaloids
Pilocarpine
Neostigmine substitute Parasympathomimetics "Cholinomimetics" }Benzopyrinium Acetycholinesterase Inhibitors Indirectly Acting { "Anticholinesterase" }Neostigmine "Prostigmine" Drug used in Alzheimer's Disease Competitive inhibitors of Ach (Galamtamine) Non-competitive Inhibitors of Ach Antagonist
~~
Compound
I Tropicamide
and cyclopentolate
J-
subs. used in urinary incontinance atropine subs Nicotine large dose Depolarizing
Antiparkinsosnial
I I Competitive
Neuromascular
'Skeletal Muscle ,-"-'re xa n ..s --1spasmolytics ...a.. __.t __ l__ . muscle relaxants '-'-'===-----1
Antinicotinic blockers ~~
: Ganglion
}-
& Nm blockers
N-M blockers
Tubocurarine
(Curare)
Gallamine (Flaxidil) Competitive (Non-depolarizing) ~--_'_---''''_---1 Atracurium Vecuronium Rocuronium Mivacurium Non-competitive (Depolarizing)
Succinylcholine
ZAGFIZIG ACADEMIC
PANELIST
Adrenaline
Noradrenaline
r1 Catecholamine
(Corlopam) (Dobutrix)
Ephederine
H Non-catecholamine
Sympathomimetics
I Amphetamine
}H Alpha
Amphetamine
Derivatives
Partially selective
lj B2Agonist
Terbutaline
I Long acting
catecholamine
Ergotamine Natural Ergot Partial - Ergot alkaloids Semisynthetic Ergot Ergometrine Dihydroergotoxine Migraine Tolazoline Phentolamine Phenoxybenzamine
Autonomic Drugs II
j
~ Adrenergic Receptor blockers
Imidazoline
Derivatives
I Beta-Haloalkylamine
Prazocin Yohimbine
Selective Selective
A 1 blockers A2 blockers
~
according to selectivity
Propanolol B1 blockers
(Indral)
B2 blockers
Sympatholytics
}-
a and B blockers Beta blockers lipophilic according to solubility hydrophilic Labetalol Pheochromocytoma (Ismalin) propranolol metaprolol nadolol atenolol
H Adrenergic
Neuron Blockers
I Alpha
Reserpine
(Serpasil)
Depolarizing
lj Ganglion
Blockers Competitive
H Centrally
- - Mindiet
ZAGFIZIG ACADEMIC
PANELIST
j antibacterial,
infection
M· f 10lCS
1-~
Locally
}-
Indirect Morphine
Y Systemic
anti-inflammatory
atropine homatropine
j mast
anti-allergic
}- ............••.~
1
J
j/1
Mydriatics
}-
1Passive
lActive
surface:
cocaine procaine
j infiltration:
parasympatholytics
----1 increase
antiarrhythmics para.mimetics
H lOP
---{ decrease
Guanethidine surgically
r
{ acute angle closure glucoma }-
dehydrating agent: Mannitol IV or Mg sulphate rectal oral carbonic anhydrase inhibitors short acting parasympathomimetics iridectomy
.T~a
ZAGFIZIG ACADEMIC PANELIST
ADH ~ ADH releaser: Nicotine, Yohimibine, Barbiturates, Morphine Thiazides only in Nephrogenic Diabetes Insipidus Choloropamide & Carbamazepine only in pituitary diabetes insipidus adrenaline, noradrenaline, dopamine in LD serotonin
} }H Anti-diuretics
} r
}
~/-[ Thiazide diuretics (Moderate efficancy)
Spironolactone
Kidney (Diuretics)
'---
{ Theophylline "Caffeine"
Methyl-Xanthines
Aldosterone antagonist
-
Triamterene Amiloride
UAcetazolamide
"Diamox"
}c_
Acidifying diuretics
ZAGFIZIG
FlCADEMIC PANELIST
Quanidine
Procaineamide
Disopyramide Aprinidine Phenytoin Lidocaine
Group A
Digitoxin
1Ouabain
I Digoxin
~~~~~~G~rO~U~p~BI~ _Iv1exiletine Tocainide Flecainide, Encainide, Indecainide, Propafenone Beta blocker propanolol,
Group esmolol
C ~
l~d~o~p~a~m~in~e~,~d~o~b~u~ta~m~in~e~ ~
Oxygen and IV fluid when needed Nitroglycerin inital nr treatment I Morphine r Frusemide Digoxin thrombolytics (fibrinolytics)
Amiodarone,
Bretylium,
Sotalol
Myocardial infarction
~ ~ ~
B-blockers
-I Nitrites
reserpine
a Methyl dopa
cvs
J
Angina Pectoris
1Ca+
channel
blockers
1-- Diltiazem
Dipyrimadol
Verapamil
Nicardipine
non-selective
moxonidine rilmedinine
selective
B1
I I
arteriodilator
H~
-{
}
'-----_______/
rt neurogenic
primary or
Direct vasodilators
H secondary
diuretics}
or hypovolemic
or oligemic
Shock
}
l-
H cardiogenic
antimacrobial
l corticosteroids
a-blocker
~
saralasin
Nifedipine Verapamil Diltiazem Nicardipine benzodiazepine
angiotensin converting
enzyme system
H septic
or hyperdynamics
f-
~
dopamine adrenal steroids
adrenaline
HCa+
channel
blocker}
1 anaphylactic +-~
antihistaminic
aminophylline
anxiolytics
drugs} blocker
Iketanserin,
5-HT2
a1 and dopamine
CVS.mma
- 24/5/2011
- Mindiet
ZAGFIZIG ACADEMIC
PANELIST
H1 Histamine receptor H2 H3
Aminoacids
r-r{ Histamine
}Histamine Antagonist
r
H1 receptor antagonist
Serotonin
1Angiotensin
Autacoids
Polypeptides
Other active polypeptide }-
1Substance P
vasoactive Intestinal Peptide (VIP) Atrial Natriuretic Peptide (ANP) Neurotensin Endothelin Interleukin (ILs) Interferon (IFN) Prostaglandins
1Kinins
HEicosanoids
ZAGFIZIG ACADEMIC
PANELIST
Orciprenaline
oral
rl Bronchodilators
Bronchial Asthma
)Parasympatholytics Methylxanthines
selective B2 agonist
Salmeterol.
Formoterol
Ipratropium Theophylline
Bromide (Atrovent)
Leukotriene
Antagonist
Cysteinyl
I 5-lipoxygenase Oi-sodium
H Anti-inflammatory
drugs
Ketotifen (aditen)
H Expectorants
& Mucolytics
Respiration
Cyanide Poisoning
~ long treatment
I Na thiosulphate
l Methylene
blue or Vit C
H short
peripheral
narcotic
low addictive
codeine,
dihydrocodeineone, narcotine,
pholcodaine
Cough Therapy
~
Mucolytics Agents
Bromhexine Carboxymethylcysteine Acetyl Cysteine alkaline expectorants sedative Expectorants )Na+ K+ Acetate, Bicarbonate, Benzoate, Citrate
stimulant
cresosote,
.T~a
ZAGFIZIG ACADEMIC PANELIST
phenanterane
group
Morphine Codeine
Papaverine L-:-B,"e'_"nz""YLr:=ls-=o~q",ui",n:=occlin-,-e'-------1r N . oscoplne Semi-synthetic Morphine derivatives =_......._........_=----='-'-=-"-'-'=-=-----j Meperidine Morphine codeine Di-Acetyl Morphine (Heroin) Apomorphine
f._'-'......."...':'.l.'.'" ......
Morphine subs.
I-
full agonist:
~ another
eNS (1)
(Analgesic Drug)
non-selective COX inhibitor
systemic use
r Acetyl
I Salicylamide
salicylic "Aspirin"
f-'-1'..""="""""".=-=.._.-o.::...:_==-_ Phenylobutazone
Non-steroidal } anti-inflammaroty -,-(N_S_A_I_D_s),--~ ~'-..._C_d:_::ru."-'g_s Indole derivatives Oxphenbutazone Indomethacin Sulindac Diclofenac
Pyrazolone derivatives
Dipyrone
Antipyretic Analgesic
}
selective COX2 inhibitor
r NSAID
I steroids
Salicylates (large dose) Probenecid in large dose Sulphinopyrazone Phenylbutazone and
Allopurinol
ong acting
ZAGFIZIG FlCADEMIC PANELIST
Phenobarbitone Amobarbitone
Pentobarbitone Secobarbitone Thiobarbitone Thiopentone Toxicity Diazepam, Cholorodizepoxide, Chlorazepate, Flurazepam, Nitrazepam, Clonazepam Oxazepam, Lorazepam, Temazepam, Alprazolam
~ Barbiturates
f-}-=':_:_::C_:_::C::_:C""-_
ultra short
Acute Barbiturate
long acting
intermediate
short
-
minor tranquilizing hypnotic according to use antiepileptic antispasticity general anasthesia advantage of benzodiazepine over barbiturates
Glutethimide
eNS (II)
Morphine
H Others l-
Thalidomide Methyprylone Ethyl Alcohol Bromide Chloropromazine Phenothiazine group Promazine Thioridazine Trifluoperazine Droperidol, Haloperidol, Trifluoperidol
r---:_:_::C_:_::_C~:=_'-'--'~_::COC_--1
Benzodiazepine
r-T-r-a-n-q-u-i-I i-z-e-r-s~}-~
Non-benzodiazepine
I Buspirone
Mepbromate
l Non Benzodiazepine
I Atropine
Anticholinergic drugs
lAntihistaminic
Tolcapone Ergolines Bromocryptine Amantidine Selegiline
Levodopa (L Dopa)
UlAntiparkinsonian Drug
}-
Dopaminergic drugs
ZAGFIZIG ACADEMIC
PANELIST
Grand Mal epilepsy Methyl-xanthines Cocaine Atropine, Amphetamine, Methylphenidate Pentylene Tetrazole Picrotoxin Bemegride (Megimide) Indirect Nikethamide (Coramine) Doxapram (Dopram) Carbogen Camphor Strychnine Spinal cord} { Hallucinogens} Dual --{ Brain stem } (Analeptics) Direct
r{ types
of epilepsy
1 stimulant
( Cerebral
Ethosuximide (Zarontin)
eNS stimulant
eNS (III)
It
I--
ID-
Acetazolamide (Diamox) Lamotrigine Vigabatrin new anti-epileptic drugs Gabepentin Felbamate Tiagabine Topiramate
Y Status Epilepticus
Tricyclic Antidepressants (TCA) ~ Old "traditional"
Lithium Carbonate ~
I J
Antidepressants
}-{
Serotonin Specific Reuptake Inhibitors (SSRI) Novel "New" Serotonin Norepinephrine Reuptake Inhibitors (SNRI) Bupropion
'{ Atypical
Trazodone
.T~a
ZAGFIZIG ACADEMIC PANELIST
Volatile liquid
Ethers Halogenated
gases
Barbiturates
General
Benzodiazepines
'f Intra-venous}Balanced
~ analgesia (induction)
~------------------~
r-
H excitement
(delirium)
N surgical
~==~-------,
medullary depression
eNS (IV)
(Anasthesia)
examination and preparation of patient
H medication proper
Pre-Anasthetic Medication
H Natural alkaloid
Local }-
cocaine
H synthetic l
J~f-=-__!__---
{ HMG CoA reducatase inhibitors bile acids binding resins { fibric acid derivatives {niacin Ezetimibe Neomycin B-Sitosterol Probucol D-thyroxin Estrogens iron deficiency anemia pernicious anemia aplastic anemia (agranulocytosis) Methemoglobinemia iron ~ chelators cyanocobalamine (vit B12) folic acid
J J
ZAGFIZIG
ACADEMIC
-.
PAN
Hyperlipidemia
interfere with ionized Ca2+ Heparin direct acting Heparin derivatives LMWHs
}
Anticoagulants }-
Coumarins Indandione
Htypes of anemia
-{
Hdrugs}
Antianemic drugs
J\
Blood
Bivalirudin
Antifibrinolytics
1/~
Coagulants
1 Systemic
{Streptokinase
r
}
}~
lVit C
Antihemophilic globulin
I Protamine sulphate
Adrenaline and
" J
}
Aspirin Dipyridamol (persantin) { Triclopidine - Clopidogrel { Abciximab - Tirofiban - Eptifibatide - Integrelin { Sulphinopyrazone (Anturan) Dextran - Heparin - Pentoxifylline Nifedipine - Clofibrate (aromid S) Prostacyclin PGI2 Blood.mma - 29/5/2011
- Mindiet
Anti-Platelet } Antithrombotic
}H
}
r
_.
~
phenmetrazine Sibutramine Orlistat
Omeprazole
I Lansoprazole
IRabeprazole
noradrenergic pathway
I Telenzapine
I Pirenzepine
Proglumide
Propantheline and
~ rf Antisecretory
sialagogues drug
1-
gastrin antagonist
I Somatostatin
I Octreotide
Prostaglandins
Misoprostol Cimetidine
--{ others
H2 blockers
j carminatives j GIT
antispasmodic cholgogues { hepatotosic drug hydrophilic granules -> Agar Saline purgatives lactulose
Peptic Ulcer
}systemic chemical
I[local
I Aluminium
I I
~ --l Physical
~ physical
I Calcium
salt
liquid paraffin dioctyl Sodium Sulphosuccinate glycerin suppositories evacuate enema figs and prunes Phenolphthalein Bisacodyl Anthacine derivatives Castar oil jalap, croton oil adn colocynth treatment of cause Bismuth, chalk, kaolin, charcoal pectin (apple and carrot) cholera severe irritant (drastic) moderate mild Lubricant
I I anion
f-
'I Eredication
--{ chemical irritant
of H. pylori Hyoscine
~
--{ Laxatives
Y
central
Antihistaminic (H1 blocker) Phenothiazine Butyrophenone Metoclopramide (primperan) Dopaminergic antagonist Domperidone (motilium) Sui pride Glucocorlicoids { Antiemetics Agents Pyridoxine (vit B6) Nabilone and Dronabinol Ondansetron dopamine antagonist peripheral prokinetics drugs Cisapride Motilin like agents Central apomorphine rapid acting slow acting Erythromycin Metoclopramide
specific treatment
adsorbants GIT protectives absorbants astrigents non specific (sympatomatic) anti-motility agent --{ treatment of } diarrhea
}-
Vomiting
Diphenoxylate (Lomotil) Loperamide (Imodium) Atropine and subs. Alkaloid of opium correction of dehydration and electrolyte disturbance
I Dompridone ~
Emetics Agents
peripheral
ZAGFIZIG ACADEMIC
PANELIST
(GH)
hormones
1types
IPituitary
Hypothalamic & Pituitary Hormones
of DM
S
~~
Pancreatic Hormones }and Antidiabetic drugs
1 Insulin receptor
Antidiuretics Oxytocin
Hormone (Pictocin)
1 Anabolic
monophasic biphasic triphasic pills pills pills
steroids
IIl
~~~ildiabetic agents
}-I
Biguanides
IllI1n~sullllllrin1_-S""eElln~s>llit[l2iz~e'r:rs'__r...:.T.:_:h,-= Acarbose
t-
I
[
combined
a-Glucosidase
Inhibitors
H Hormonal
Contraceptives
1 Thyroid
Parenteral
Iodine
Aldosterone Desoxycorticosterone Hydorcortisone prednisolone· methyl prednisolone· Dexamethazone (D.O.C) short acting Minrelacorticoids ~
Parathyroid glands
Hypoparathyrodism Hyperparathyrodism
+ cortisone
prednisone
triamcinolone . Betamethazone
Ad renocortical hormones
~-------~
j 1Calcitonin
L1
1Vitamin
D hormone
Parathyroid
Raloxifene Danazol
1Non
hormonal
agents
Mifepristone
Anti-Progesterone
Testosterone androsterone
Progesterone
ZAGFIZIG ACADEMIC
PANELIST
Spectrum
}-
Streptomycin Chloramphenicol
I Tetracyclines
lQuinolones
}1 kill bacteria '1 inhibit bacteria
ability
{ cell wall r
synthesis inhibitors
I--
I
General Chemotherapy
Macrolide antibiotics Clindamycin
I Clarithomycin
Erythromycin
'-------,--------~____j{
I azithromycin
Streptomycin
mechanism
of action
}-
I--
I Gentamicin
I Neomycin
& Kanamycin
indirect
Polymixin B
}-
~ Antibiotics
I Cepalosporins
I Aminoglycosides
Nitrofurantoin Nalidixic acid Mandelic acid Methamine
y Antiseptic f-
~
--{ respiratory virus infection }
ZAGFIZIG
FlCADEMIC PANELIST
-.
Amantidine Rimantidine
Ribavirin Interferon Lamivudine Adfovir Entecavir Acyclovir Herpes nucleoside and nucleotide reverse transcriptase inhibitor (N RTls) treat AIDS non nucleoside reverse transcriptase inhibitors (NNRTls) protease inhibitors Dapsone Clofazimine Leprosy Isoniazid virus infections --{ hepatic viral infection
1Nystatin
}
}
1Amphotericin
Antifungal
H Antiviral
}-
1Flucytosine
{ Imidazole derivatives
1Griseofulvin
H HIV
infection
r r
{ Antituberculous }-
r r H Anti-Malaria
}
Special Chemotherapy
furoate 8 Hydroxyquinolines
Chemo. of Amebiasis
}-
I Antibiotic
Halogenated
}
}
r r r
Metronidazole,
Mebendazole,
Pyrantel
pamoate,
Albendazole
1Praziquantel
Anti-bilharzial drug
Mebendazole,
Abendazole
}H Anti-Helminthics
}- H
H Oxamniquine
Metrifonate
H Niridazole
Praziquantel,
Praziquantel,
~ Dimercaprol
ZAGFIZIG ACADEMIC PANELIST
K Di-Sodium
Chelating Agents
'-------_______/
Edetate
K Dicobalt edetate
D-penicillamine
Hypokalaemia
H causes }-
Miscillaneous
impaired renal function 82 blockers and digitalis 81 blockers and NSAI Ds ACEI (Captopril) Succinycholine Spironolactone Acidosis Hypoaldosteronism
Miscillaneous.mma - 30/5/2011 - Mindiet
Hyperkalaemia
Hcauses }-