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Pharm > Pharm terms (Block 1) > Flashcards

Pharm terms (Block 1) Flashcards

1
Q

How are drugs classified?

A
  1. Based on their main effect (analgestics)
  2. Based on their clinical/therapeutic use (antivirals)
  3. Based on their mechanism of action (beta-blockers)
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2
Q

Drug size & molecular weight

A
  • Less than a 100 not selective for receptors
  • Greater than a 1000 poorly absorbed & poorly distributed
  • Smaller = BETTER
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3
Q

Chemistry of Drugs

A
  • Inorganic
  • Small/large organic

-Bio macromolecules = recombinant proteins, antibodies, polysaccharides, nucleic acids

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4
Q

Stereoisomers

A
  • 1/4 to 1/2 of all drugs exist as this
  • same molecular formula and sequence of bonds BUT different 3D shape
  • Structural isomer = same molecular formula, BUT bonded together in different orders
  • Racemic mixture of drug’s steroisomer
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5
Q

Pharmacokinetics

A

-What does the body do with the drug

  • Absorption
  • Distribution
  • Metabolism/Biotransformation
  • Elimination
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6
Q

Enteral administration

A
  • Delivery of drugs via GI tract
  • Oral, sublingual, rectal
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7
Q

Pareneteral administration

A

-Delivery NON GI tract

-Injections (most common) Subcutaneous, Intradermal, Intramuscular, Intravenous

-Cutaneous: Topical or transdermal (systemic)

-Mucous membrane: Eyedrops, ear drops, throat sprays, inhaled, vaginal, urethral

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8
Q

Bioavailability

A
  • quantitative measurement of drug absorption also called volume of distribution (VD)
  • fraction of a drug dose reaches systemic circulation unchanged
  • Each drug possess different bioavailability depending on route of admin.

-IV is 100% bioavailability

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9
Q

What are the 3 major areas that drugs are administrated?

A

-Therapeutic sites: tissues/organs where drug can function

-Tissue réservoirs: tissues/organs where drug can be stored (drug depot)

-Unwanted sites of action: Tissues/organs where drug is able to elicit unwanted effects this leads to adverse effects/toxicities

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10
Q

Drug metabolism, Biotransformation, Clearance

A
  • May activate, inactivate, or maintain drug activity
  • Major organ involved is liver
  • Major enzyme involved cytochrome P450 (located in smooth endoplasmic recticulum of hepatocytes)
  • Clearance = majority Renal OTHERS are intestines, lungs, skin, sweat
  • Quanitative measurement = Clearance of drug (CL)
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11
Q

Pharmacodynamics

A

-What Drug does to the body

  • Study of the effects, actions, and mechanisms of drug
  • Receptors, mediators, targets, toxicity
  • Binding of drugs to receptors done by non-covalent bonds (hydrogen, ionic)
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12
Q

Pharmacodynamics (Mech of Action)

A
  • Molecular mods cause pharm action of drug
  • Drugs do NOT interact with organ as a whole BUT w/molecules in tissue
  • Drug receptors = bio macromols (reg. proteins, ion channels, cell surface, carrier proteins)
  • Drugs binding to receptors = noncovalent bonds (H bonds, van de waals, ionic)
  • Non covalent = Specific / selective & reversible action
  • Covalent = less specific & irreversible
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13
Q

Pharmacodynamics (Bound drugs)

A
  • Full agonist - Drug when bound = activates receptor to produce MAX response
  • Partial agonist - Drug when bound = activates receptor to produce BELOW max level
  • Antagonist - Drug when bound = fails to completely to make activate receptor
  • Inverse agonist - Drug when bound to active receptor (intrisic or basal activity) decreases basal activity
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14
Q

Pharmacodynamics (Drug interaction)

A
  1. Mechanism of action - Drug X functions as a full agonist of Beta-receptors
  2. Pharmacological action - (functional or physio effect) Drug X increases frequency of spontaneous depolarization of SA node
  3. **Pharmacological effect - (observed effect) **Drug X induces tachycardia
  • Drugs targeting self - primary use to manipulate physio of body
  • Drugs targeting NON-self - Chemotherapy or target other foreign organisms in body
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15
Q

Pharmacodynamics (Contraindications & Precautions)

A
  • Condintion makes use of drug INADVISABLE
  • Absolute contraindication = makes use of drug absolutely inadvisable under ALL circumstances
  • Relative contraindication = makes use of drug SOMEWHAT in advisable BUT does not rules it out (precaution)
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16
Q

Pharmacodynamics (Reproductive Toxicity)

A
  • Teratogenic = Effect in the uterodevelopment of organism resulting in abnormal structure or function. NOT heritable
  • Mutagenic = Effect on inheritable characteristics of cell/organism. Mutations in DNA
  • Ames test-invitro = test for mutagenicity & carcinogenesis
  • Dom. lethal test-invivo = males exposed to substance & observed for progeny (Offspring)
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17
Q

Schedule 1-5 Drugs

A
  1. Heroin, LSD, Cannabis, peyote, EX - NO current medical use in US
  2. Hydromorphone, oxycodone, fentanyl, morphine, adderal - High potential for abuse (narcotis/Stimulants)
  3. Vicodin, high dosage of tylenol, Ketamine, steroids, benzphetamine - Moderate/low dependence or HIGH physio dependence
  4. Xanax, klonopin, diazepam, lorazepam - LOW potential abuse
  5. Cough syrup or has limited narcotics (100 ml of codeine per 100 grams)- LOW abuse potential
  • Analogs - drugs whose structure is related to another drug BUT pharm & chem properties differ
  • Congener- Drug made by same chem rxns & same pharm effect
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18
Q

Route of Admin (Enteral & Parental)

A
  • Enteral- Sublingal, oral, buccal, rectum
  • Mouth, Stomach, SI (big SA & most drugs absrobed here), Colon, rectum
  • Parental- Injections, pulmonary admin, cutaneous admin, mucoud membrane
  • Used for drugs poorly absorbed in GI tract, QUICK onset, HIGH bioavailability
  • Can cause local tissue damage = Nerve damage in subcutenous injection
19
Q

1st pass effect

A
  • Prodrugs use to their benfit
  • Greater the 1st pass the LESS the agent will reach the systemic circulation when administered orally
  • Primary enzymes affect metab = GI lumen, Gut wall, bacterial, hepatic
  • Oral preps - Enteric coated = chem envelope resists action of fluids & enzymes in stomach BUT dissolve in Upper Intestine & Extended release = Special coating control how fast drug is released to body
20
Q

Pharmcokinetics (Drug absorption)

A
  • Acidic drugs (HA) release a proton (H+) = charged anion to make = A-
  • Basic drugs (Bh+) release proton causing UNCHARGED base = B
  • **Uncharged substances can cross hydrophobic cellular membrane **
  • **Charged is better excreted **
  • Conc of permeable form of drug is determined by ratio of carged to uncharged forms
  • Ratio = Depends on PH absorption site & ionization constant (pKa)
  • LOWER pka = more acidic
  • HIGHER pka = more basic
21
Q

Ion Trapping

A
  • Body fluids vary in PH difference from blood PH will favor trapping or reabsorption
  • Small intestine
  • Breast Milk
  • Aqueous humor
  • vaginal secretions
  • prostatic secretions
  • Acidic drugs are ionized (charged) = cant cross membrane MOST found in urine
  • Basic drugs concentrated in LOW ph enviroment = Gastric bile
22
Q

Determinants of drug absorption

A
  • P-glycoprotein - transmembrane transporter protein expressed through out body, when HIGHLY expressed reduces drug absorption
  • Functions = Liver (transports bile for excretion)
  • Kidneys (pumps drugs into urine)
  • Placenta (transports drugs into maternal blood)
  • Intestines (transports drugs into lumen & reduces drug absoption into blood)
23
Q

Volume of distrubution (Vd)

A
  • Vd=Amount of drug in body / plasma drug conc @ time 0 or (X/C0)
  • A drug binds to blood components remains confined to blood & has small volume distrubution
  • Drugs that have extra-vascular tissue binding have large VD
  • Plasma compartment = Drugs w/large mol weight or drugs that bind to plasma proteins are TRAPPED
  • Extracellular fluid = Low Mol weight drugs are hydrophilic can move into interstitial fluid, BUT no crossing lipid
  • Total body water = Low mol weight drugs hydrophobic move across cell membrranes
  • HIGH AVD values = 100-1000’s long 1/2 life use loading doses
24
Q

BBB

A
  • Tighter endothelial arrangement leaving NO gaps
  • Absence of transport systems & membrane channels
  • Presence of acid pumps (like in kidney) active transport out of CNS into blood
25
Q

Special Tissues

A
  • Placenta = Drugs w/ mol wt. less than 1000 daltons & moderate high lipid cross barrier w/Simple diffusion
  • Blood-cerebrospinal fluid = HIGH lipd soluble drugs can cross - CSF barrier
  • Testis = Tight junctions between sertoli cells - restricts passage of drugs to spermatocytes & spermatids
26
Q

Phase 1 metabolism

A
  1. Functionalization rxns
  2. Converts parent drug to more POLAR by introducing finctional group (OH, NH2)
  3. Results in loss of pharm activity
  4. = or more active than parent
  5. Almost all oxidative enzymes local to endoplasmic reticulum
  • Mixed function enzymes found in microsomes of many cells - performs diff functions rxns
  • Oxidation, reduction, hydrolysis, hydration
  • If compound is NOT completely secreted THAN on to phase 2
27
Q

Phase 2 metab

A
  • Conjugation rxns
  • Enzymes located in cytosol
  • RXNS:
  • Glucuronic acid (glucuronidation)
  • Sulfate (sulfation)
  • Acetic Acid (acetylation)
  • AA (glutathione/glycine conjug.)
  • Alkyl group (methylation)
  • HIGHLY polar - rapidly excreted in urine/feces
  • Usually inactive - exception morphine
28
Q

Cytochrome P450

A
  • Metab of diverse endogenous & exogenous compounds
  • Drugs, enviromental chems, xenobiotics (chem found in body not normally produced)
  • Catergorized into 17 families (cyps#) 40% identical
  • Subfamilies 55% identical CYP#A, B, C
  • Isoforms CYP#A#
  • St. John’s wort INDUCES P450
  • Grapefruit inhibits P450
29
Q

Biliary Excretion

A
  • Similar to kidneys (ACTIVE)
  • Lipid soluble drugs filter intially, get reabsorbed along with water, NOT excreted effciently
  • Acid/Bases active secretion WORKS effectively if MW high enough
  • Conjugation to glucoronide increase MW for bilary excretion
30
Q

Zero & 1st order kinetics

A
  • 1st order = amount of drug metabolized or excreted in given period of time DIRECTLY proportional to PLASMA conc. 1/2 life is constant
  • Zero order = Saturation kinetics = ehtanol. Constant amount of drug eliminated PER unit time
31
Q

Pharmacodynamics (receptors)

A
  • Drugs can INHIBIT enzymes - enzymes control # of metabolic processes, very common mode of action
  • Drugs BIND to - Proteins, genome (cyclophosphamide), microtubules (Vincristine)
  • Receptors located - IN or ON cells, tight bonds w/ligand, requirements (size,shape,stereospecificity), signal transduction
  • Proteins act as - Regulatory, enzymes, transport, structural
32
Q

Pharmcodynamics (Drug interaction)

A
  • Affinity = measurement of drug binding to receptor - covalent = STRONG/irreversable & Electrostatic bonds = strong or weak/reversible.
  • Inverse of Kd like Km 1/2 max binding
  • Efficacy (intrisic activity) = ability of drug to change the receptor in a way that MAKES an effect, SOME drugs have affinity BUT no efficacy
  • Like Vmax and closer to Y axis = MORE efficacy
33
Q

Second Messengers

A
  • Small, nonprotein, water-soluble
  • Rapidly spread thoughout cell by DIFFUSION
  • C-AMP - reg. protein phospho -
  • Ca+2 ions - more common than C-AMP used in NT, GF
  • Increases in Ca+2 = Muscle contraction, secretion, cell division
34
Q

Spare Receptors

A
  • Max drug response obtained @ less than max occupation of receptors
  • NOT qualitatively different from NON-spare receptors
  • Effect may presist longer than interaction
  • Insulin = 99% are spare & Beta on heart
  • Compare Max binding (kD) with conc (Ec) w/spare receptors
35
Q

Agonists & Antagonists

A
  • Agonist - Binds to receptor directly or indirectly = FULL activation of effector systems
  • Partial agonist - makes LESS than full effect EVEN when saturated receptors, acts as inhibitor in presence of full agonist
  • Antagonist- BINDS no activity to receptors = BLOCKS or competes w/agonist
  • Repeated admin of agonist or antagonist = changes in responsiveness @ receptor
  1. Down-regulated
  2. Endocytosis inside cell
  3. Unresponsive to ligand
  • Inert binding site = Albumin (no effect when bound)
36
Q

Comp. Antagonists

A
  • Competes w/agonist receptor
  • Binds reversibly w/o activating effector system
  • Atagonists increase agonist conc needed for REPONSE
  • CONC-effect curve shift to HIGHER doses
  • Effects are overcome by adding MORE agonist
  • Increases median effective dose = ED50
  • Irreversible antagonist = more dependent on turnover of receptors & works w/spare receptors
37
Q

Graded Dose Response

A
  • Relationship between drug & receptor is graded
  • Continuous & gradual
  • Semi-logrithmic plots due to range of doses & conc. can vary = sigmodial shape
  • Potency = EC50 amount of drug needed to make effect - use 50% of max dose
  • Smaller the value for EC50 greater the potency
  • Efficacy = Emax magnitude of drug effect can cause at max dose = ALL receptors occupied= NO reponse with dose increased
  • Potent drugs = make less of demand on metabolic enzymes = lesser side effects
38
Q

Drug receptor binding

A
  • Law of mass action - Relationship between drug conc & receptor occupancy (insertion of 1 mol will NOT alter binding of other mols)
  • **DR/Rt = D/Kd + D **
  • DR = conc of bound drug
  • D = Conc of free drug
  • _Rt = t_otal conc of receptors (bound & unbound)
  • Kd = dissociation constant of receptor for drug
39
Q

Dissociation constant (Kd)

A
  • Strength of interaction between ligand & receptor = conc of drug required to bind 50% of receptors
  • Kd= D*R/DR
  • HIGH Kd = weak interaction & low affinity
  • LOW Kd = strong interaction & high affinity
  • Mag of response is proportional to amount of receptors bound or occupied
  • Emax = all receptors bound
  • binding of receptors exhibits NO cooperativity
  • E/Emax = D/Kd+D (E=effect on drug conc (D))
40
Q

Effectiveness, Toxicity, Lethality

A
  • ED50 = Median effective dose (dose which 50% of pop manifests given effect)
  • TD 50=Median Toxic dose (dose which 50% of pop manifests toxic effect)
  • LD50 = Letal dose (dose which kills 50% of subjects)
  • Theraputic index = Ratio of TD50 or LD50 to ED50
  • Increased index = wider margin of safety (represents safety of drug)
  • Ex of safe drug is very LARGE toxic dose & small effective dose (ED50 of 3mg & LD50 of 150mg)
  • Theraputic window = doage range is minimum effective conc (MEC) & max toxic conc (MTC)
  • Ex. MEC = 7-10mg/L (average 8mg/L) & MTC = 15-20mg/L (average 18mg/L) = Window 8-18mg/L
  • Warfarin SMALL theraputic index & Penicillin LARGE theraputic index
41
Q

Frequency of Distrubution

A
  • NOT cumulative
  • Plots # of responders @ each dose increment OR dose LVL (conc)
  • Bimodal response curves = heterogeneity in pop w/respect to response of drug
42
Q

Terminology of Drig Effects

A
  1. Side effects = Not intended or desired, Minor problem
  2. Adverse effects = Undesirable, more serious
  3. Toxic effecets = Serious undesired effects, potentially FATAL
  • On target = excessive actions, Inappor conc, suboptimal kinetics, incorrect tissue (Diphenhydramine + H1)
  • Off target = Effects unrelated to action, binds to unintended receptor (Terfenadine + Cardiac K+ channel)
43
Q

Idiosyncratic Rxns

A
  • G6PD def - 6-phosphogluconate synthesis via G6PD produces NADPH required maintaining GSH LVLs
  • When LACKING cannot protect against RBC oxidative stress = G6PD def
  • Protect against maleria
44
Q

Hypersensitivities 1-4

A
  1. Immediate hyper - atophy, anaphylaxis, asthma - Mediators (IgE)
  2. Antibody mediated hyper - Autoimmune, hemolytic anemia - Mediators (IgG or IgM)
  3. Immune complex mediated hyper - Serum sickness, Lupus - Mediators (IgG)
  4. Delayed hyper - Transplant reject, dermatitis, tuberculosis - Mediators (Tcells, macrophages, histocyctes)

Pharm (14 decks)

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