M&M PharmPrinciples Flashcards by Stanley Danso

Process by which drug moves from site of admin to bloodstream

Absorption

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Absorption is influenced by characteristics of drugs such as

Solubility
Pka
site of absorption
dose

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Fraction reaching systemic circulation is

Bioavailability

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Preferentially absorbed form of the drug is

nonionized

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Acidic environment favors Absorption of (AAA)

Acidic drugs

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Basic environment favors ABSORPTION of

Basic drugs

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This route may be limited by first pass metabolism by the liver

Oral

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Routes bypasses liver and first pass metabolims

SL or buccal

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Provide prolonged continuous administration

Transdermal

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What is the effective barrier to all but SMALL, highly potent lipid soluble drugs

Stratum Corneum

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SC and IM injection depends on what

Diffusion from the site of injection to the circulation

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During SC and IM , diffusion from the site of injection to the circulation depends on what

Blood flow to the area
Carrier vehicle

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Which one is absorbed faster, solution, or suspensions?

SOLUTIONS

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Irritating preparations can causes

pain and tissue necrosis

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IV injections and absorption

Bypasses the process of absorption because the drug is placed directly into the bloodstream

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The process of circulation of a drugs in the blood throughout the body is

Distribution

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Name all the highly perfused organs?

Brain
Heart
Liver
Endocrine glands
Kidneys

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Less perfused organs are? what is the significance?

Fat and skin ; equillibrate more slowly because of low blood flow.

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What law do drug molecule obey?

law of mass action

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Explain the law of MASS ACTION that drug molecule obey? (Gradient)

When plasma concentration exceeds the concentration in tissues, drugs moves from plasma to tissue. When the plasma concentration is less than the concentration in the tissue, drugs moves from TISSUE back to PLASMA

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Binds many acidic drugs what protein?

Albumin

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Binds many BASIC drugs what protein

Alpha 1 acid glycoprotein (AAG)

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Diseases where albumin is decreased?

Renal
Liver,
Chronic CHF
malignancies

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Alpha 1 acid glycoprotein (AAG) are increased in

TRAUMA( including surgery)
Infection
MI
Chronic pain

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Alpha 1 acid glycoprotein (AAG) are decreased in

Pregnancy

The apparent volume into which a drugs has been distributed is called its

Volume of distribution (Vd)

How is Vd determined?

dose divided by concentration : Vd = Dose/concentration

Most anesthetic drugs are lipophillic or hydrophillic

liphophillic

Most anesthetic drugs are liphophillic resulting in a Vd that

Exceeds total body water .

What is total body water?

~ 40 L

The Vd of fentanyl is about

350L

The Vd of propofol may exceed

5000L

The chemical alteration of a drug is the ______aka____

biotranformation; metabolism

Primary organ of metabolism

liver

The primary end products of metabolism characteristics?

INACTIVE and WATER SOLUBLE

What drugs characteristics allows excretion by the kidney?

WATER SOLUBLE

Metabolism can be divided into 2 reactions

Phase I and Phase II

What happens during phase I reaction? name them

Convert drugs into a MORE POLAR metabolites through Oxidation, reduction or HYDROLYSIS

What happens during phase II reaction? name the process involved?

Phase II couples or CONJUGATE a parent drug or a phase I metabolite with an ENDOGENOUS SUBSTRATE, to form a water-soluble metabolites that are eliminated in urine or stool.

Example of endogenous substrate that may be used by phase II reaciton

GLUCORONIC ACID

Can a phase I metabolites be excreted without undergoing PHASE II biotransformation?

YES

Can a Phase II reaction precede or occur without a phase I reaction?

YeS

Volume of plasma of blood CLEARED of drug per unit of time is

HEPATIC CLEARANCE

What is hepatic clearance?

BLOOD FLOW times the HEPATIC EXTRACTION RATIO Clearance = Q x E

What is the hepatic extraction ratio?

Fraction of drug entering the liver that is metabolized.

If the extraction ration is 50%, what is hepatic clearance

It is half of liver blood flow.

Principal organ of excretion

Kidneys

Kidneys: explain what happens with ionized and unionized fraction of the drug?

Ionized fraction of Drug EXCRETED IN URINE NONionized fraction of drugs get REABSORBED in the RENAL TUBULES

What part of kidney are nonionized drugs absorbed at

RENAL tubules.

The rate of elimination of a drug from kidney excretion is the

Renal clearance

Renal clearance formula

Clearance = Q x E (renal extraction ratio)

What is enterohepatic circulation?

DRUG excreted into the bile and THEN REABSORBED in the intestine

Multi-compartment models provide

Mathematical framework to relate drugs dose to a drug concentration overtime

2 compartment drug model phases

Distribution or ALPHA phase Elimination or BETA phase

Explain the distribution or alpha phase

After an initial bolus , there is a RAPID drop in concentration over the first few minutes as drugs quickly DIFFUSES into PERIPHERAL compartments

2 compartment graph explanation x-axis Y-axis SHAPE

X-axis is the --> TIME after dose y-axis is the --> PLASMA Concentration STEEP drop then slow downward slope

Explain the Elimination or beta phase

Continued drop in concentration but LESS STEEP decline in plasma concentration

What is pharmacodynamics

How drugs affects the body

Concepts of pharmacokinetics are

ADME Absorption Distribution Metabolism Excretion

Concepts of PHARMACODYNAMICS are (PET)

POTENCY EFFICACY Therapeutic window

What does the dose response curve explain?

relationship between drug dose and pharmacologic effect

The shape of drug dose and pharmacological effect is

SIGMOIDAL in a log scale.

The sigmoidal shape of the dose response curve means that

a certain amount of drug must be present before there is any measurable physiologic response.

The left side of the dose response curve is flat until

the drug concentration reaches a minimum threshold.

The right side of the dose response curve is flat until

reflecting the MAXIMUM physiological response of the body.

What is the therapeutic window defined as

Difference between the concentration associated with a desired therapeutic effect and the concentration associated with a toxic drug response.

Therapeutic index is

Toxic concentration / therapeutic coencentration

What are drug receptors usually made of

Usually macromolecules typically proteins that bind a drug and mediate the drug response.

Bind a drug

Agonist

Reverses the effects of the agonist

Antagonist

Occurs when the ANTAGONIST competes with THE AGONISTS for the binding site , each displacing the other.

COMPETITIVE ANTAGONISM

WHEN the ANTAGONISTS through COVALENT BINDING or another process PERMANENTLY impaired the drug's access to the receptor?

NONCOMPETITIVE ANTAGONISM

Drugs effect is governed by what?

FRACTION of receptors occupied

Fraction of receptors occupied is based on

concentration of drug Concentration of a receptor AFFINITY of drug to the receptor.

What is the RECEPTOR occupancy importance

the first step in mediating the drug effect.

Binding of a drug to a receptor can trigger MULTIPLE STEPS including

opening or closing of ion channel activating of a G protein activating an intracellular kinase Interaction directly with a cellular structure, binding directly to DNA

Prolonged binding and activation of a receptor may lead to (PROLONGED AGONIST)

HYPO reactivity (desensitization) and TOLERANCE

If the binding of Endogenous ligand is chronically blocked, receptors may proliferate, resulting in (PROLONGED ANTAGONIST)

HYPERREACTIVITY and INCREASED SENSITIVITY.

Beta-blockers cause subtype-specific upregulation such that nonselective beta-blockers increase the density of both.

beta1- and beta2-adrenoceptors whereas beta1-selective antagonists upregulate only beta1-adrenoceptors

Chornic BETA blockers, As a consequence of increased sympathetic tone, cardiac beta-receptors are down-regulated in the

failing ventricle and dilated cardiomyopathy.

However, in the presence of acute myocardial ischemia there is rapid upregulation of beta-receptors in the presence of _____________which forms the basis of beta blockade therapy for treatment of ACS.

elevated circulating catecholamines,