Pharmacology Lecture 1

Polypharmacy

the regular use of 5 or more medications at the same time

Pharmacology

A broad study of drugs and meducation including action mechanism, parameters for pharmacokinetics and pharmacodynamics, interactions, adverse and toxic effects

Pharmacotherapeutics

combines pharmacology of medication and concept of how to use the medication in patients with various disease states

Pharmacodynamics

mechanism of action (what the drug does to the body)

Pharmacokinetics

what the body does to the drug (ADME)

Receptor

specific target for medication to attach and exert its effect

Agonist

med. binds to receptor and activates it (structures match)

Antagonist

med. binds to receptor without activating it (blocks the receptor/structures don't match)

Drug Side Effect

known or expected possible reactions (range from mild to moderate)

Drug Adverse Effect

unintended, undesirable or potentially harmful potential responses (typically more severe)

Drug Allergic (Hypersensitivity) Reaction

an unpredictable immune-mediated reaction (range from mild to severe)

Define Enteral Administration with methods

drug absorbed through the GI system (oral/sublingual, topical/transdermal, and rectal)

Define Parenteral Administration with methods

drug that bypasses the GI tract (IV, IM, SC or inhalation)

Define Systemic Drugs

a drug that reaches the bloodstream and circulates throughout body despite administration method

Brand Drugs

- patented name for first to make/discover the medication

- usually more expensive

Generic Drugs

- one/internationally recognized name

- nonproprietary and usually less expensive

- available to make after patent expires

Describe the Autonomic NS

controls involuntary bodily functions

-can be influenced by thought and emotion

Describe Sympathetic NS.

aka. Noradrenergic - fight, flight, freeze (exercise, excitement, emergency and embarrassment)

What impacts Sympathetic NS? (chemicals/receptors)

norepi and epi exerts actions on alpha and beta receptors

Describe Sympathomimetics and what drugs cause it.

agonists to sympathetic NS (adrenergic & pressors)

Describe Sympatholytics and what drugs cause it.

antagonist to sympathetic NS (Beta-blockers and Alpha-blockers)

Describe Parasympathetic NS.

aka. cholinergic - rest and digest (Digestion, defecation and diuresis)

What impacts Parasympathetic NS? (chemical/receptor)

acetylcholine on nicotinic and muscarinic receptors

Describe Parasympathomimetic and what drugs cause it.

agonists to parasympathetic NS; cholinergic agents

Describe Parasympatholytic and what drugs cause it.

antagonists to parasympathetic NS; anticholinergic agents

What are the adrenergic Receptors?

G-protein coupled receptors (alpha 1, alpha 2, beta 1, beta 2)

What drugs impact all Autonomic NS receptors?

adrenergic agonists

what drugs impact Alpha 1 NS?

adrenergic agonists and sympathomimetics

what drugs impact Alpha 2 NS?

adrenergic agonists and sympatholytics

what drugs impact Beta 1 and Beta 2 Receptors?

beta blockers (adrenergic agonists)

What are the 3 General Pregnancy Categories?

1. Pregnancy (L&D)

2. Lactation (nursing mothers)

3. People of Reproductive Potential

What is Involved In Pregnancy Category 1?

submit to pregnancy exposure registry and look at risk summary, clinical considerations and known data

What is Involved In Pregnancy Category 2?

Look at risk summary, clinical considerations and known data

What is Involved In Pregnancy Category 3?

Need a pregnancy test, know contraceptive agents and look at infertility risks

What is a controlled Drug?

a drug that manufacturing, possession and use are regulated by law(DEA); requires authorization for use d/t abuse schedule

Describe the 5 schedules of a controlled drug.

I - harmful, not considered medically necessary, only used in research (heroin)

II - more likely to be abused (narcotics, MMJ, ADHD meds)

III - safer, less likely to be abused (codeine products)

IV - safer, less likely to be abused (tramadol, benzos, sleep agents)

V - safest, least likely to be abused (expectorants with codeine)

ADME

absorption, distribution, metabolism and excretion

BLA

Biologics License Application

CADD

computer-aided drug discovery

DEL

DNA-encoded compound library

DHHS

U.S Department of Health and Human Services

DMPK

drug metabolism and pharmacokinetics

FBDD

fragment-based drug discovery

FDA

U.S. Food and Drug Administration

GPU

Graphics Processing Unit

HCV

hepatitis C virus

HDL

high-density lipoprotein ("good" cholesterol)

HMG-CoA

3-hydroxy-3-methyglutaryl coenzyme A

HTS

high-throughput screening

IND

Investigational New Drug

LDL

low-density lipoprotein ("bad" cholesterol)

mRNA

messenger RNA

NDA

New Drug Application

NIH

National Institutes of Health

NMEs

new molecular entities

PDUFA

Prescription Drug User Fee Act

SBDD

structure-based drug design

siRNA

small interfering RNA

PO

by mouth

List General Timeline of Drug Development

- Discover/Preclinical Period

- Phase 1 (Clinical Trials)

- Phase 2 (Clinical Trials)

- Phase 3 (Clinical Trials)

- Regulatory Review Period

- Phase 4 (Post-Marketing Surveillance)

Describe New Drug Discovery/Preclinical Phase (in terms of animal, human, duration and cost)

Animal Testing - extensive

Human Testing - none

Duration - 3-6 years

Cost - $10-100 million

Describe new drug Phase 1 (in terms of animal, human, duration and cost)

Animal - data from previous phase

Duration - months-1 year

Cost - $1-10 million

Human - 20-100 healthy volunteers in specific centers; focus on safety, toleration, interactions

Describe new drug Phase 2 (in terms of animal, human, duration and cost)

Animal - limited/if needed

Duration - 1-2 yrs.

Cost - $10-100 million

Human - 100-300 patients with target disease; focus on efficacy, side effects and optimal dosing

Describe new drug Phase 3 (in terms of animal, human, duration and cost)

Animal - few, unless new safety concerns show

Duration - 2-4 yrs.

Cost - $100-500 million

Human - 1000-3000 across multiple sites; foxus on efficacy confirmation, adverse reaction monitoring, preparing data

Describe new drug Regulatory Review Period (in terms of animal, human, duration and cost)

Animal - none

Duration - 6 months-2 years

Cost - $2-5 million

Human - none, submitting data in NDA

Describe new drug Phase 4 (in terms of animal, human, duration and cost)

Animal - rare

Duration - indefinite

Cost - varies

Human - ongoing monitoring of patients in real-world use