Pharmacology Lecture 1

Pharmacology

The study of drugs, actions, and reactions

Pharmacokinetics

What the body does to the drug, how a drug moves through the body

Pharmacodynamic encompasses what three things

Desired therapeutic response, physiologic changes, and adverse reactions/toxicities

Pharmacodynamics

What the drug does to the body, the biological and physical changes the drug causes

Pharmacokinetics encompasses what 5 things

Absorption, Distribution, Metabolism, Excretions (ADME), and can also include accumulation/toxicity

As a drug concentration increases _____ is reached

maximal effect- Emax

Potency is defined as ____

EC 50

Potency can only be used to compare drugs that are what

in the same drug class

Can potency of drugs in different classes be compared?

NO

The smaller dosage it takes to reach EC50 the ____ the potency

higher

The larger the dose it takes to reach EC50 the _____ the potency

lower

______ response includes a degree or range of responses that varies with the dose

Graded

______ response is the average effect of a drug as a functions of concentration. “all or nothing”

Quantal

Graph can be interpreted as the % of the number of patients responding

Quantal

Which is more potent and why? KnockoutPAM 0.5 or SleepiPAM 5mg

KnockoutPAM 0.5, it takes a smaller dose to reach efficacy

What is the therapeutic index

The concentration/dose required to produce the desired therapeutic effects, below toxicity

What is the therapeutic window

The dosing room that elicits the desired effect before we hit toxicity

What does it mean when drugs have a small therapeutic index (dosing range)

The therapeutic dose is only slightly above the non-effective dose and slightly below toxicity

With a narrow TI small dose changes can produce big __________ changes

concentration

What is the formula for therapeutic index

Therapeutic dose 50 (TD50) / Effective dose 50 (ED50)

When a receptor is blocked this results in a ________ of receptor production

upregulation

what are some types of medications that are an alpha-1 agonist

Vasopressors and decongestants

____ agonist are used with asthma and COPD. They result in the relaxation and dilation of smooth muscle

Beta

What are the three opioid receptors

Mu, Kappa, and Delta

The ___ receptors are opioid receptors that provide analgesia, sedation, and euphoria. BUT have the side effects of respiratory depression, Miosis (pinpoint pupils) and physical dependence

Mu

The ___ receptors are opioid receptors that provide alagesia with minimal respiratory depression BUT often have the side effects of dysphoria and miosis

Kappa

The ___ receptors are opioid receptors that provide analgesia BUT have the side effect of Modulation of hormone and NT release

Delta

_________ is required in some drugs due to the ability of the cell to upregulate or downregulate the density of receptos

dose tapering

What effect does an agonist have after it binds the receptor

mimics the natural or typical action of a neurotransmitter/ other endogenous agent

What type of agonist is used to stimulate smooth muscle relaxation, used in asthma and preterm labor contractions

Beta-two

What type of agonist stimulates vasoconstriction to help with low BP levels due to sepsis, or in common decongestants for stuffiness

Alpha-one

What happens after an antagonist binds the receptor

It blocks or weakens (attenuates) the natural response to the neurotransmitter or endogenous chemical

What type of antagonist lower blood pressure by blocking vascular constrictions

Alpha-one

Beta blockers ___ the heart rate by blocking receptors from stimulating NTs

Slow

What type of antagonist blocks the action of histamine in the stomach, thus reducing acid secretion

Histamine-2

What happens when partial agonist binds the receptor

elicits a sub-maximal/ weaker response

partial agonist may also block the natural action of NTs/chemicals and attenuate and agonist response. When can this be helpful

over-active endogenous conditions

what is an example of a medication that acts as a partial agonist

Buprenorphine

What are some common reasons why knowing what receptors drugs work on is important

impact test/therapy, influence exercise tolerance, mask diagnostic testing, mask response to hypogylcemia, hypotension, falls, N/V

What are some common di/trivalent cations that may affect drug-food interactions

Calcium, Magnesium, aluminum

what is one medication that has bad adverse effects when mixed with alcohol

Metronidazole (Flagyl)

What are some possible pharmacodynamic interactions

antagonistic (dec effect), additive/synergistic (inc effects)

What are some red flag medications that should signal you as the provider to check for drug interactions

Transplant (anti-rejection), HIV, HCV, seizures, warfarin, and anti-psychotics

If a drug is Category A what does that mean

Human studies have proven the drug is okay in pregnant women

If a drug is Category B what does that mean

Animal studies have proven minimal risk in pregnant women

If a drug is Category C what does that mean

Animal studies show some risk, no human studies, but benefits might outweigh the risks so use clinical judgement

If a drug is Category D what does that mean

DON’T, evidence of human risk, rare cases may have benefit

If a drug is Category X what does that mean

Absolutely do not use, benefits do not outweigh the risks

For drugs after what year are you provided with a narrative vs categories

2018