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14-PHARMACOLOGY
receptor
ligand gated/ch link/ionotropic(fastest)
GABAAR(open Cl ch), nAChR, 5HT3R, GlyR
Gprot coupled/metabotropic
shape-serpentine(7memb)
Gprot-GDP couple with Alp(Active),, subunit
adenyl cyclase pathw(cAMP)
Gs(adr)
Gi(M2,M4,2adr,adr antag)
cAMP-TSHR, FSHR, LHR, ACTHR, PTHR, glucagonR, calcitoninR, adrenalineR,
vasopressinR(V2)
cAMP-DR
phospholiase C pathw(IP3,DAG)
Gq(M1,M3,M5,1adr)
Gt(transducin)-generate signal in rod
small Gprot(monomer)-Ras prot
enzyme linked
insulinR(tyrosine kinase), GHR(janase kinase), prolactin(janase kinase), cytokineR,
ANFR(cGMP), NO(cGMP)
intracellular(slowest)
Cytoplasmic-Corticosteroid, mineraloCorticoid
nucleus-testosterone, E, vitA&D, thy h
grp I-nuclear recept
grp II-surf recept
2nd messenger
hydrophobic-DAG,IP3
hydrophilic-cAMP,cGMP
gas-NO,CO,H2S
clinical trial(HECP)
0-microdosing
I-Human pharmacology
Healthy Human volunteer
safety&tolerance
ADR
pharmacodynamic
pharmacokinetic
II-therapeutic Exploration
Efcacy
III-therapeutic Conrmation
Comparision with established drug
IV-Postmarketting suveillance
ADR/toxicity
pharmacogenetic-genetic basis for variable response
pharmacogenomics-genetic information to guide DOC
pharmacognosy-drug fr plant
pharmacovigilance-detection, assessm, understand, prevent ADR
pharmacodynamic&pharmacokinetic
0 order kinetic indep of-pl conc
ED50-potency
area under time&pl conc-pl clearance
loading dose-vol distribution
maintenance dose-clearance
chloroquine, digoxin, doxycycline, long acting sulfonamide, phenylbutazone,
lignocaine(short t)
Li excreted by kidn, not metab
oscillatory response-+ve feedback
entrOPy not change-OPen system
biotransformat rxn
phase I(non synth) rxn
oxidation(MI-cytP450), reduction, hydrolysis, cyclization, decyclization
phase II(synth) rxn
acetylation, glucuronide conjugation, Gly conjugation, SO4 conjugation, methylation,
nucleotide synth
less polar more polar
bioavailability
extensive 1st pass metab-oral route
drug-bioavailability(%)
bisphosphonate,remelteon=2
furosemide=60
sotalol,pindolol,penbutolol=100
Acidic drug-Albumin
basic drug-1glycoprot
preparation-drug
capsule
hard-tetracycline
soft-vitE
sustain release-theophylline
time release-indomethacin
depot preparation-flupentixol, fluphenazine, haloperidol, imipramine, risperidone
ETT-adrenaline, atropine, diazepam, naloxone, lignocaine
ID-BCG vacc
inhaler
aerosol-salbutamol, beclomethasone
dry powder-salbutamol
gas-GA
spinhaler-diNa chromoglycate
desmopressin, liposome, butorphanol, zanamivir, calcitonin
intravitreal-bevacizumab, foscarnet, ganciclovir, ranibizumab, pegaptanib
nasal spray-sumatriptan
SC-sumatriptan, morphine, vitB3, exenatide
SL-isosorbide diNO3, buprenorphine, ergot amine tartrate, isoprenaline,
nitroglycerine, desaminooxytocin, clonidine, nifedipine
suppository-diclofenac, indomethacin, aminophyllin, diazepam, metronidazole,
chlorpromazine, bisacodyl, glycerine, morphine, ergotamine, paracetamol
tablet
chewable-ergotamine tartrate, acarbose, Al(OH)3, Mg trisilicate
double strength-cotrimoxazole
enteric coated-bisacodyl
mouth dissolving-ondansetron
sugar coated-metronidazole
sustain release-pyridostigmine, morphine, diclofenac, theophylline, pinacidil,
prazosin, pentoxyphylline
uncoated-amlodipine
transdermal-fentanyl, nicotine, nitroglycerine, estradiol, hyoscine, rotigotine
ability of vehicle to retard evaporation fr skin
ointment> foam> cream> paste> powder> aerosol> gel> lotion> wet dress> tincture
liposome
anticancer drug-daunorubicin, vincristin, camptothecin, mtx, cisplatin, mitoxantron
antifungal-amphotericinB, nystatin
antibiotic-amikacin, ampicillin, ciproflox, ribavirin, ganciclovir, chloroquine
other-IL2, cyclosporine
food
tobramycin-Streptomyces tenebrarius
drug causing hemolysis in G6PD def
A-Aspirin
D-Dapsone
Na-Nalidixic acid
N-Nitrofurantoin
Sami-Sulfonamide
Pe-Primaquine,Phenacetin
M-Menadione(vitK3)
C-Chloroquine
Q-Quinine
drug causing hyperpigmentation(CCAM)
Chlorpromazine
Clofazimine
Amiodarone
Minocycline
drug causing disulram like rxn
C-Chlorpropamide, Cefoperazone, Cefamandole, Citrate Ca carbamide, Cyanamide,
animal Charcoal
M-Metronidazole
Praised-Procarbazine
G-Griseofulvon
T-Tinidazole
Naidu-Nitrofurantoin
drug causing deafness(BEDEAFM2C2Q)
Bleomycin
Ethacrynic acid
Desferoxamine
Erythromycin
Aminoglycoside
Furosemide
Minocycline
Mustine
Chloroquine
Cisplatin
Quinine
enzyme inducer
G-Griseofulvin
P-Phenytoin
R-Rifampicin
S-Smoking
Cell-CBZ
Phone-Pnenobarbitone
enzyme inhibitor
Vitamin-Valproate
K-Ketoconazole
Cannot-Cimetidine
Cause-Ciprofloxacin
Enzyme-Erythromycin
Inhibition-INH
grape fruit juice
drug metab by acetylation(SHIPCD)
Sulfonamide
Hydralazine
INH
Procainamide,PAS
Clonazepam
Dapsone
fAsT acet-hepATiTis
sLOw acet-peripheraL neurOpathy
drug with low therapeutic index
V-Vancomycin
C-Clonidine
D-Digoxin
P-Phenytoin
Layer-Lithium
G-Glipizide
I-Imipramine
F-Flucytosine
T-Theophylline
drug with 0 order kinetic
Zero-Zidovudine
W-Warfarin
A-Aspirin
T-Theophylline
T-Tolbutamide
Power-Phenytoin
MBCMIC-bactericidal
warfarin
INR=ptPT/contrPT=2-3, prosthetic valve=2.5-3.5, long term=1.5-1.9
paracetamol does not
stimulate respiration
affect acid base balance
cause gastric irritation
have CVS affect
affect PLT fn
cause uricosuria
pethidine(meperidine)
hydrolysis meperidinic acid(maj), inh by MAOI producing more demethylation
demethylat norpethidine(min) sz
opioid recept
endorphin(),enkephaLin(DeLta)
P-Physical dependence,Prolactin
M-Miosis
C-Constipation,Convusion(M3G)
A-Analgesic(spinal,supraspinal)
R-Resp depression
E-Euphoria
S-Sedation
Dynorphin()
D-Dysphoria
M-Miosis
A-Analgesic
R-Resp depression
D-Diuresis
S-Sedation
Muscle rigidity-Mu
digitalis
toxicity-hypokalemia, hypercalcemia, hypermagnesemia, ren failure
CFTR
corrector-lumacaftor-correct trafcking defect
potentIator-Ivacaftor-open Cl ch
drug act on
tamoxifen
E antag-Breast,Bld vess
E agonist-uterus,bone,lipid
dopamine
dose(g/kg/min)-action
low(1-2)-renal&mesenteric vasodilat
moder high(2-10)-1adr agonist, +ve ionotropic
high(>10)-1adr agonist, vasoconstrict
steroid
0mineralocort-triamcinolone, paramethasone, dexamethasone, betamethasone
0glucocort-DOCA(DeOxyCorticosterone Acetate)
most potent glucocort-betamethasone
least potent glucocort-cortisone
max mineralocort-aldosterone> fludrocortisone> DOCA
max glucocort-dexa&betamethasone
hydrocortisone:prednisolone:dexamethasone= 1:4:40
advantage 2nd gen antihistam
less-sedation, interaction with alcohol, psychomotor disturb
FDC malaria-artemether+lumefantrine
Abbreviations
a-artery, AA-amino acid, abtc-antibiotic, AI-autoimmune
bef-before, bel-below, b/l-bilateral, bld-blood, b/n-between, bn-benign, br-branch,
Bx-biopsy
ca-carcinoma, carb-carbohydrate, c/i-contraindication, c/l-contralateral,
conc-concentration, cong-congenital, Cx-cervix
d-day, def-deficient, ds-disease, d/t-due to, Dx-diagnosis
E-estrogen
fem-female, fr-from
gld-gland, glu-glucose
h-hormone
idiop-idiopathic, i/l-ipsilateral, inf-infection, inj-injury
lig-ligament, LL-lower limb, l/t-leading to
m-muscle, maj-major, mal-male, MC-most common, met-metastasis, min-minor,
mtx-methotrexate, Mx-management
n-nerve, norm-normal
P-progesterone, pl-plasma, prot-protein, pt-patient
Rx-treatment
SCC-squamous cell carcinoma, sr-serum, Sx-surgery, sz-seizure
tm-tumour, ts-tissue
UL-upper limb, u/l-unilateral
vag-vagina, VC-vocal cord, vel-velocity, vert-vertebra, vit-vitamin, vol-volume
w-week, wt-weight
Xr-X ray
y-year
#-fracture
-degree
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