Principles of Pharm Flashcards

1
Q

What is Pharmacotherapeutics?

A

Drugs used to prevent, treat, or diagnose a disease
-composed of 2 components: pharmacodynamics and pharmacokinetics

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2
Q

What is Pharmacokinetics?

A

The study of how a drug is absorbed, distributed, or eliminated from the body

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3
Q

What is Pharmacodynamics?

A

The analysis of what a drug does to the body at the systemic and cellular levels
-what the effect the drug has on the body
-the effect of the substance on biological substances

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4
Q

What are the 3 different names a single drug can have?

A
  1. Chemical: the compound the drug is made of
    ex: propionic acid
  2. Generic: official name
    ex: ibuprofen)
  3. Trade or Brand: assigned by the pharmaceutical company the drug was manufactured from
    ex: Celebrex
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5
Q

Why use the generic named drug over the brand named drug?

A

Generic drugs are often substituted for a brand name drug because they are cheaper. However, they need to be tested to ensure the 2 drugs are equal (same amount of active ingredients, same absorption, and same metabolism). Even if the drugs are equal, some patients have more side effects or different reactions to the generic drug.

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6
Q

Phases of drug testing on humans

A

Phase 1: tested on 10-100 healthy subjects
-pharmacokinetic parameters established
Phase 2: tested on 50-500 subjects with the specific disease
-clinical benefits and range of toxicities determined
Phase 3: tested on several hundred to thousand subjects
-safety and efficacy established

**typically takes 4-6 years of testing to gather all data

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7
Q

Drug Approval Process

A
  1. testing on animals
  2. testing on humans (Phases 1-3)-
  3. if animal and human testing meets expectations, an application is submitted to the FDA for approval - which can take 3+ years
  4. label made IF approved by FDA
  5. marketing of the drug (Phase 4)- monitoring the safety of the new drug (no fixed duration)

*time from filing for a new drug for approval to when marketing begins can be 5+ years

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8
Q

What is the lifetime of a patent?

A

In the US a patent lasts 20 years in which only the owner of the patent can manufacture the drug. After the 20 years, any company has the ability to make said drug without paying license fees to the original owner

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9
Q

What is Off-Label Prescribing?

A

Physicians can prescribe drugs for reasons other than what that drug is originally intended for
Example: Gabapentin which is used for seizures can also be effective in pain management

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10
Q

The Controlled Substances Act

A

Places drugs in specific categories based on their likelihood of addiction of abuse. Restrictions exist for how often a patient can refill their prescriptions to prevent abuse.

Categories: schedule I, schedule II, schedule III, schedule IV, schedule V

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11
Q

What does is the Dose-Response Curve? What is threshold and ceiling effect?

A

Provides information about the dosage range where the drug is effective
-threshold dose: minimum dose to cause cellular changes
-ceiling effect: any doses above this level will not result in any further changes

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12
Q

What is Potency?

A

The amount of drug needed to produce a given effect
-the more potent a drug, the less of that drug is needed to achieve the desired therapeutic effect
Example: if drug A produces a desired effect at a much lower dosage compared to drug B, then drug A is more potent.

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13
Q

Median Effective Dose

A

The concentration of the drug at which 50% of the population responds to it in the expected manner
Example: 50% of people who take a pain killer experience absence of pain

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14
Q

Median Toxic Dose

A

The dose at which 50% of the population exhibits the specific adverse effect

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15
Q

Median Lethal Dose

A

The dose that causes death in 50% of the animals it was tested on

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16
Q

Therapeutic Index (TI)

A

This is an indicator of a drug’s safety and it is determined by the median effective dose and the toxic dose (TI= toxic dose/median effective dose)
-the higher the TI, the safer the drug because it indicates that it takes a higher dose of the drug to evoke a toxic response
-blood levels should be monitored for drugs with low TI values to ensure there is no toxicity occurring
Example: OTC drugs have a higher TI than prescription drugs

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17
Q

Examples of Different TI Values

A

-Tylenol: 27
-Demerol (narcotic analgesic): 8
-Valium (sedative): 3
-Chemotherapy Drugs: 1
**the low TI of cancer drugs is accepted because some of the toxic effects of the drug outweigh the risk of not taking the meds

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18
Q

Enteral Administration

A

A form of taking a drug which involves the GI system
Examples:
-oral
-sublingual
-bucal
-rectal

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19
Q

Parenteral Administration

A

A form of taking a drug that does not involve the GI system
Examples:
-inhalation
-injection
-topical
-transdermal

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20
Q

What is the most common enteral method?

A

Orally- swallowing the drug where it is absorbed from the GI lumen- typically absorbed within the small intestine and transported to the liver, then taken to their action site

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21
Q

What must a drug be for it to be effectively absorbed within the GI tract?

A

Must be lipid soluble so it can pass through the GI mucosa and into the bloodstream. If it is not lipid soluble there will be poor absorption and it will be eliminated from the body

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22
Q

What are the advantages and disadvantages of taking a drug orally?

A

Advantages: easy, convenient, safe

Disadvantages: stomach irritation, potential breakdown of drug by stomach acid, absorption may be slower, absorption is less complete than some parenteral routes, first-pass effect

23
Q

What is the First Pass Effect?

A

When a significant amount of a drug taken orally is metabolized by the liver before it ever reaches its site of action

24
Q

How to avoid the first-pass effect of oral meds?

A

Make sure the dose of the drug is great enough to take the first-pass effect into consideration. Although some drugs cannot be taken orally if the first-pass effect is too great

25
Q

What is so beneficial about being able to take drugs either sublingually or buccally?

A

These drugs are not subject to the first-pass effect of the liver, meaning they will not be metabolized by the liver
Example: nitroglycerin is taken sublingually because it will not be destroyed by the liver if taken orally

26
Q

Advantages and Disadvantages of rectal administration

A

Advantages: able to be used if patient is unconscious or cannot swallow, partially avoids the first-pass effect

Disadvantages: poor absorption, incomplete absorption, and irritation of rectal mucosa

27
Q

Overall Advantages of Parenteral Administration

A

-deliver drugs to the action site more directly
-quantity of the drug that reaches the site is more predictable
-not effected by first-pass effect of liver

28
Q

Inhalation Administration

A

Drugs are inhaled via aerosol form and it travels to the alveoli where they diffuse into the pulmonary circulation- can cause some irritation to the alveoli or respiratory tract

29
Q

Different Types of Injection

A

-IV: into peripheral vein which allows for an accurate quantity to reach the bloodstream quickly
-Intra-arterial: into artery to allows a large dose of a drug to go directly to the targeted organ with limited exposure to other tissues (chemotherapy)
-Subcutaneous: directly below the skin to allow drugs to be absorbed slowly into bloodstream
-Intrathecal: delivered within a sheath (subarachnoid space), tendon sheath, or bursa

30
Q

Topical Administration

A

Drug is applied to the surface of the skin or mucous membrane that is used to treat conditions on the skin- not well absorbed across the epidermis and into the systemic system
Examples: wound healing, anti-inflammatories for skin inflammation, eye drops, and ear drops

31
Q

Transdermal Administration

A

Applying drugs directly to the surface of the skin for the drug to be absorbed into the subcutaneous tissues or peripheral system (opposite of topical drugs). These drugs must be able to penetrate the skin and not be affected by the enzymes within the dermis
Examples: medicine patches (nicotine, hormone, pain), iontophoresis, phonophoresis

32
Q

Advantages of Transdermal Drugs

A

-allows for a slow controlled release of a drug
-allows for a specific medication to be administered through the skin to a muscle, tendon, or bursa

33
Q

What is Bioavailability?

A

The extent to which a drug reaches the systemic circulation
-given as a percentage of the amount of the drug administered
Example: 50% bioavailability- when 100 mg of a drug is taken orally and only 50 mg reaches the blood stream

34
Q

What factors Affect Bioavailability?

A

-route of administration
-ability of the drug to cross various membranes
-distribution to peripheral tissues from the systemic system to reach a target site

35
Q

What factors affect the distribution of drugs?

A

-tissue permeability
-blood flow
-plasma proteins
-sub-cellular components

36
Q

Lipid-Soluble vs. Nonlipid-Soluble drugs

A

Lipid soluble drugs are able to reach all different body components and enter every cell they reach whereas nonlipid soluble drugs will remain in the compartment or tissue where it was administered due to a cell’s lipid layer keeping them out

37
Q

Blood Brain Barrier

A

This barrier limits the movement of drugs out of the blood stream and into the CNS tissues

38
Q

What is the significance of certain drugs binding to plasma proteins?

A

There will be some drugs that will form irreversible bonds to plasma proteins within the blood stream which essentially results in that portion of the drug becoming ineffective
-only unbound drugs can reach a target tissue and produce the desired effect

39
Q

Why do some drugs bind to sub-cellular components?

A

Certain drugs bind to sub-cellular components in order to trap the drug within that specific cell so it cannot travel to any other cells to have an effect
Examples: anti-depressants and antipsychotics

40
Q

What is meant by volume distribution (Vd)?

A

A ratio of the amount of the drug taken over the concentration of the drug within the plasma
(Vd= amount of drug/concentration in plasma)
-used to estimate how well a drug was distributed throughout the body
-can have more concentrations in different tissues (blood, bone, fat)

41
Q

Where within the body can storage occur?

A

When drugs are not eliminated rapidly, they may be stored in body tissues after being absorbed
-adipose tissue
-bone
-muscle
-organs

However. high concentrations of drugs in adipose tissue, bone, muscle, or organs can be detrimental

42
Q

Why do some people have prolonged effects from drugs or prolonged side effects?

A

Storage sites/tissues that have stored a drug may leak the drug out later after drug levels within the plasma has decreased

43
Q

What are controlled-released substances and what are the advantages?

A

Drugs that are designed to have a slower and prolonged absorption rare from the GI tract or other routes

Advantages: less doses needed per day, prevents large fluctuations of the amount of drug in the plasma, and allows for steady plasma levels over night

44
Q

What are the two ways drugs are eliminated from the body?

A
  1. Biotransformation: when a chemical change occurs that alters the drug so it is inactive
  2. Excretion
45
Q

What are the different types of biotransformation?

A

-oxidation: when either oxygen added or hydrogen is removed
-reduction: when oxygen is removed or hydrogen is added
-hydrolysis: the drug compound is broken down into parts by enzymes
-conjugation: drug joins with other another substance, such as amino acids

46
Q

What is the most common type of biotransformation?

A

Oxidation

47
Q

What does most biotransformation occur?

A

the liver

48
Q

What is drug tolerance?

A

When there is prolonged drug use the body adjusts and destroys the drug more rapidly which results in needing to increase the dosage for it to have the same effect

49
Q

What are the different sites for excretion?

A

-kidneys are the primary site
-lungs
-GI tract
-sweat
-saliva
-breast milk

50
Q

Elimination Rules

A

-if a drug is administered faster than it is eliminated, the drug will accumulate within the body
-if a drug is eliminated faster than administration, then the therapeutic effect level will never be reached

therefore, the dosing of a drug depends on knowing the rate at which the drug will be eliminated

51
Q

Clearance

A

When a drug has either been eliminated from the system or from a specific organ. It is based on the blood flow to the organ and the fraction of the drug that is removed from the plasma as it passes through the organ
-if an organ has poor blood flow, then clearance will be decreased

52
Q

What is half-life?

A

The amount of time required for 50% of the drug in the body to be eliminated
Examples: Acetaminophen has a half-life of 2 hours, so every 2 hours 50% of the drug within the body will be eliminated

53
Q

What factors affect how an individual responds to drugs?

A

-genetics
-disease: damage to an organ affects drug metabolism or excretion
-drug interactions
-age: older patients are more sensitive to drugs
-diet: total calories and types of calories affects absorption and metabolism
-sex: men and women metabolize differently
-exercise
-smoking
-alcohol
-obesity
-SCI