Predominant Binding of Proteins of Drugs

download Predominant Binding of Proteins of Drugs

of 14

Transcript of Predominant Binding of Proteins of Drugs

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    1/14

    PREDOMINANT BINDING OFPROTEINS OF DRUGS

    ALBUMINCeftriaxone (A)CCelecoxib (N)Citalopram (B)Clofibrate (A)Dexamethasone (N)Diazepam (B)Diazoxide (A)CDiclofenac (A)Diflunisal (A)CDicloxacillin (A)Digitoxin (N)Etodolac (A)Etoposide (N)CFenoprofen (A)Fluoxetine (B)Flurbiprofen (A)dFluvoxamine (B)

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    2/14

    Ibuprofen (A)c,dIndomethacin (A)Itraconazole (N)Ketoconazole (N)Ketoprofen (A)dKetorolac (A)dLosartan (A)Meclofenamate (A)Mefenamic Acid (A)Meloxicam (N)Mycophenolic acid (A)Nabumetone (N)C

    Nafcillin (A)Naproxen (A)COxacillin (A)Oxaprozin (A)Paroxetine (B)Phenylbutazone (A)CPhenytoin (A)Piroxicam (A)Prednisolone (N)C

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    3/14

    Probenecid (A)Rifapentine (A)Rofecoxib (N)Salicylic acid (A)CSertraline (B)Sulfisoxazole (A)Sulindac (A)Teniposide (N)Thiopental (A)CTiagabine (A)Tolbutamide (A)Tolmetin (A)Valproic acid (A)CWarfarin (A)d

    ALBUMIN AND AAGAlfentanil (B)Alprenolol (B)dAmprenavir (B)Carbamazepine (N)

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    4/14

    Clindamycin (A)cCocaine (B)cDisopyramide (B)b,c,dErythromycin (B)Fosphenytoin (A)Lidocaine (B)Lopinavir (B)

    Meperidine (B)Methadone (B)dNelfinavir (B)Olanzapine (B)Perphenazine (B)Prazosin (B)Propafenone (B)Quinine (B)Ritonavir (N)Ropivacaine (B)Saquinavir (B)Triflouperazine (B)Verapamil (B)d

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    5/14

    ALBUMIN, AAG, AND LIPOPROTEINS

    Amitriptyline (B)Amphotericin B (N)Bupivacaine (B)dChlorpromazine (B)Diltiazem (B)Docetaxel (N)Felodipine (N)Imipramine (B)Nortriptyline (B)Paclitaxel (N)Perazine (B)Propranolol (B)dQuinidine (B)

    ALBUMIN AND LIPOPROTEINSAmiodarone (B)Cyclosporine (N)bProbucol (N)

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    6/14

    Conversion

    Units

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    7/14

    AvoirdupoisUseful EquivalentsLength1 inch = 2.54 cm1 meter = 39.37 inVolume1 fluidounce = 29.57 ml1 pint = 16 fl.oz (473 ml)1 quart = 32 fl.oz (946 ml)1 gallon = 128 fl.oz (3785 ml)1 gallon, UK = 4545 mlWeight1 ounce = 437.5 grains1 pound = 16 ounce

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    8/14

    ApothecariesUseful EquivalentsVolume1 fluidrachm/fluidram = 60 minims1 fluidounce = 8 fl.dr (480 minims)1 pint = 16 fl.oz1 quart = 2 pints1 gallon = 4 quartsWeight1 scruple = 20 grains1 dram = 3 scruples1 oz = 8 dram1 pound = 12 oz

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    9/14

    DOSE FORMULAS

    Youngs Rule, based on ageDose of Child = X Adult dose

    Cowlings Rule=

    Frieds Rule for infants=

    Clarks Rule, based on weight=

    AgeAge + 12

    Dose ofChild

    Age at next birthday (in yrs.) X Adult doseXAdultdose24

    Dose forInfants

    Age (in months) X Adultdose150

    Dose ofChild

    Weight (in lbs.) X Adult dose150 (average weight of adult in lbs.)

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    10/14

    Dose Based on Body Weight= Patients Weight (kg) X

    Dose Based on Body Surface Area

    = X Drug Dose (mg)

    =

    PatientsDose (mg) Drug dose (mg)1 (kg)

    PatientsDose (mg) Patients BSA (m

    2)1.73 m2

    PatientsBSA (m2) Patients height (cm) X Patients weight (kg)3600

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    11/14

    pH negative logarithm of Hyrdronium ionconcentration

    pH Normality interms ofHydroniumIonNormality interms ofHyrdroxyl Ion

    0 1 10-14

    1 10-1 10-132 10-2 10-12Increasing 3 10-3 10-11acidity 4 10-4 10-105 10-5 10-9

    6 10-6 108Neutral point 7 10-7 10-78 10-8 10-6

    9 10-9 10-5

    10 10-10

    10-4

    11 10-11 10-3Increasing 12 10-12 10-2alkalinity 13 10-13 10-114 10-14 1

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    12/14

    pKa Values of Some Common DrugsDrugs pKa value

    Acidic drugsAspirin 3.5

    Paracetamol 9.5

    phenobarbital 7.4 (first

    ionization)

    Basic drugs

    Cocaine 8.6

    Diazepam 3.3Diphynhydramine 90

    Amphoteric drugs

    Morphine 8.0 (amine),

    9.9 (phenol)Adrenaline

    (epinephrine)

    8.7 (amine),

    10.2, 12.0

    (phenols)

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    13/14

    FOR WEAK ACIDS

    pH = pKa compound is approximately 50%

    ionized

    pH = pKa +1 compound is approximately 90%

    ionized

    pH = pKa + 2 compound is approximately 99%

    ionized

    pH = pKa +3 compound is approximately 99.9%

    ionizedPh = pKa + 4 compound is approximately 99.99%

    ionized

    FOR WEAK BASES

    pH = pKa compound is approximately 50%ionized

    pH =pKa compound is approximately 90%

    ionized

    pH = pKa compound is approximately 99%

    ionized

    pH = pKa compound is approximately 99.9%ionised

    pH = pKa compound is approximately

    99.99% ionised

  • 7/28/2019 Predominant Binding of Proteins of Drugs

    14/14