Introduction to Pharmacology, Drug Discovery, Routes of Administration Flashcards

1
Q

Define generic, brand and chemical name of the drugs

A

Generic: Derived from the chemical name and non proprietary
Brand: Assigned to the compound by the pharmaceutical company
Chemical: refers to the specific compounds structure

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2
Q

What are Schedule I drugs?

A

Schedule I: Drugs or chemicals with no currently accepted medical use with the high potential for abuse
Heroin, LSD, Weed, MDMA

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3
Q

What are Schedule II drugs?

A

Schedule II: drugs or chemicals with a high potential for abuse with accepted medical use, can lead to severe psychological or physical dependence
Methylphenidate, methamphetamine, oxycodone, morphine, methadone, hydromorphone, fentanyl, cocaine

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4
Q

What are schedule III drugs?

A

Schedule III: Moderate or lower abuse potential compared to schedule II
Anabolic steroids, testosterone, codeine, ketamine

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5
Q

What are Schedule IV drugs?

A

Schedule IV: Lowest potential for abuse and lower risk of dependence
Diazepam, Lorazepam, Phenobarbital, Propoxyphene, tramadol

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6
Q

What are Schedule V drugs?

A

Schedule V: Lowest abuse potential
Low dose opioids in cough meds, lamotil, pregabalin

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7
Q

What is Pharmacology?

A

Pharmacology is a broad umbrella term that encompasses pharmacotherapeutics and toxicology.
Pharmacotherapeutics can be further divided into pharmacokinetics and pharmacodynamics.

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8
Q

What is pharmacokinetics?

A

What the body does to the drug (ADME)
Absorption
Distribution
Metabolism
Excretion

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9
Q

What is Pharmacodynamics?

A

what the drug does to the body
MOA
Dose Response
Effects
SE
ADRs

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10
Q

what is pharmacodynamics dependent on?

A

Depends upon drug receptors and the ability of the drugs to bind to those receptors

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11
Q

what factors affect absorption?

A

Bioavailability is affected by stomach acidity, gastric emptying, surface area, GI enzymes, and developmental changes

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12
Q

what is bioavailability? What factors affect it?

A

The extent to which a drug reaches systemic circulation
Routes of administration
Ability to cross the membrane

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13
Q

What is toxicology?

A

the branch of science concerned with the nature, effects, and detection of poisons.

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14
Q

what factors affect drug distribution?

A

tissue permeability, blood flow, binding to plasma protein, binding to sub cellular components

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15
Q

Describe Phase-I and Phase-II drug metabolism

A

Phase I: convert a parent drug to a polar active metabolite through unmasking or insertion of a polar functional group (CYP450)
Phase II: convert the parent drug to a polar inactive metabolite via conjugation of subgroups (sulphates, glycine, acetylation, methylation)

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16
Q

With regard to drug metabolism, what are CYP inductors and CYP inhibitors?

A

Induction: Rifampin, Carbamazepine
Inhibition: Valproic acid, Fluoxetine

17
Q

Describe absorption of drugs in Infants

A
  • less stomach acid which increases bioavailability
  • delayed gastric emptying which increases the time to reach therapeutic concentration
    -larger relative skin surface area which increases cutaneous perfusion
  • thinner stratum corneum increases absorption of topicals
18
Q

Describe absorption, distribution, and excretion of drugs in the elderly

A

A: increased gastric PH and delayed gastric emptying increases the time to reach therapeutic concentrations
D: decreased TBW to 53% and increased body fat and decreased serum albumin binding
E: decreased glomerular filtration and tubular secretion (main reason for adverse reactions!)

19
Q

What is half life?

A

The amount of time required for 50% of the drug remaining the in the body to eliminated

20
Q

Active vs Passive Transport

A

Active: Minerals, sugars, and amino acids move against a concentration gradient with an input of energy
Passive: Water and water soluble substances (urea and glycerol) and small lipids move with a concentration gradient

21
Q

What are the major organs of drug metabolism and excretions?

A

The liver is the major organ that metabolizes drugs
The kidney is the major site of drug elimination and drugs are excreted in the urine

22
Q

What is Dose Response?

A

Provides information about the dosage range over which the drug is effective, provides information on peak response

23
Q

What is potency?

A

the dose that produces a given response in a specific amplitude

24
Q

What is median effective dose?

A

E50
Dose at which 50% of the population responds to the drug in a specific manner

25
What is median toxic dose?
T50 Dose at which 50% of the group exhibits the adverse effects
26
what is median lethal dose
L50 The dose that causes death in 50% of the group
27
what is therapeutic index?
The therapeutic index is the indicator of the drugs safety. The greater the TI, the safer the drug. A greater TI indicates that it takes a large dose to have a toxic response. TI=TD50/ED50 (median toxic dose/ median effective dose)
28
what is efficacy of a drug?
The efficacy of a drug is its ability to produce the maximal response possible for a particular biological system and relates to the extent of functional change that can be imparted to the receptor by the drug, based on its affinity for the receptor
29
What is drug affinity?
It tells us how attracted a drug is to its receptors.
30
Define Agonist, Partial Agonist, Mixed agonist/antagonist, Antagonist
Agonist: Drugs that occupy receptors and activate them Partial agonist: does not evoke a maximal response or fully activate a receptor Antagonist: Drugs that occupy receptors but do NOT activate them. They block receptor activation by agonists. Mixed antagonist and agonist: Simultaneously stimulate receptor subtypes while blocking other receptor subtypes
31
Compare and contrast competitive and non-competitive antagonist
A competitive antagonist binds to the same site as the agonist but does not activate it, thus blocks the agonist's action. A non-competitive antagonist binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor.
32
Drug development and Approval: Preclinical Testing
1-3 years animal trials provide preliminary info on PK and PD properties of the compound
33
Drug development and Approval: Human Clinical Testing
6-8 years Phase I: is it safe? Pk? Phase II: Does it work in patients? Phase III: Does it work double blind?
34
Drug development and Approval: Phase IV
Post marketing surveillance is on going
35
What are the various routes of administration? Which are subject to first pass?
Enteral: oral, sublingual, rectal, buccal (ORAL SUBJECT TO FIRST PASS) Parental: inhalation, injection, topical, transdermal
36
what is first pass effect?
Oral drugs are subject to the first pass effect. It is a phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation. mucous membrane of the stomach--> portal vein --> liver and metabolized