Pharm Exam 1
Chapter 2
Agonists- drugs that produce a response
o Ex) Beta adrenergic agonist: epinephrine
Antagonists- drugs that prevent or block a response
o Ex) Beta adrenergic blocker: metoprolol
Half-life- the time it takes for one half of a drug concentration to be eliminated from the body
Therapeutic Index (Window)- the level of the drug between the minimum trough concentration in the plasm a
for obtaining desired drug action and the minimum peak concentration
o Peak- the point at which plasma drug levels are the HIGHEST
o Trough- the point at which plasma drug levels are the LOWEST
Loading dose- given to achieve a rapid concentration
A patient on two highly protein-bound drugs is at risk for accumulation of one or both drugs and toxicity.
Tolerance- a decreased responsiveness over the course of therapy which may lead to the need to increase
dosages to attain the same effect
Drugs in the same class share many common features, it is extremely helpful to learn drugs by their
classifications
Drugs can be in a class with other drugs because…
o The drugs are related by their chemical structure
o The drugs work in the same way
o The drugs are used for the same purpose
Pharmaceutic Stage: ONLY TABLETS & CAPSULES GIVEN PO
o This is the process by which the tablet/capsule becomes a solution to pass the membrane of the
stomach or small intestines
Pharmacokinetic Phase: the process of drug MOVEMENT through the body to achieve drug action
o Absorption: movement of the drug into the bloodstream after administration
Most oral drugs are absorbed through the action of mucosal villi in the small intestines
Fat-soluble (lipid soluble) & Non-Ionized drugs are MOST EASILY absorbed by the GI tract
PARENTERAL DRUGS DO NOT PASS THROUGH THE GI TRACT
o Distribution- the process by which the drug becomes available to body fluids and body tissues from the
bloodstream
Affected by rate of blood flow, the drug’s affinity to the tissue, and protein binding
Protein binding- some drugs have a HIGH affinity for binding to the plasma proteins while others
have a LOW affinity to binding
Warfarin & furosemide HIGH
Lisinopril & metoprolol LOW
Drugs that are STUCK onto proteins AREN’T FREE to go to their target and do their job
Portion that remains FREE is the ACTIVE DRUG
2 highly protein bound drugs fight for binding sites leaving more FREE DRUGS leading to
accumulation & toxicity
Low PROTEIN (ALBUMIN) DECREASES binding sites
o Metabolism/biotransformation- the process in which the body chemically changes drugs into a form that
can be excreted
LIVER IS THE MAIN SITE OF METABOLISM
FIRST PASS EFFECT-also called hepatic 1st pass
Drugs are altered by passing through the intestinal lumen into the portal vein into the
liver
This is the reason some drugs CANNOT be given PO
, Bioavailability- the % of the administered dose that reaches systemic circulation (%
available for activity)
HALF-LIFE- the time it takes for the amount of drug to be reduced by ½
Affected by the amount of drug administered, the amount of drug remaining,
metabolism, & elimination
DRUGS WITH A ½ LIFE >24H SHOULD NOT BE GIVEN MORE THAN BID (DIGOXIN &
COUMADIN)
o Excretion/Elimination- process by which the drug is excreted
Kidneys, lungs, bile, saliva, sweat, breast milk
o Pharmacodynamics- onset, peak and duration of action
Onset- the time until minimum effective action/concentration
Peak- when the drug reaches its HIGHEST blood concentration
Duration of action- the length of time the drug produces a therapeutic or pharmacologic effect
o 7 MECHANISMS OF ACTION
Stimulation- fight or flight responseadrenergic drugs
Depression- decrease neural activityseizure & pain drugs
Irritation- noxious effectastringents
Replacement- replace body compoundsinsulins and hormones
Cytotoxic action- kill invading cancers or parasiteschemo
Antimicrobial action- prevent, inhibit, kill infectious organismsantibiotics
Modification of immune status- modify, enhance, depress immune systemmethotrexate
o Drug Names
Generic- chosen by a variety of official bodies
Usually are r/t the chemical components of the drug
Brand- chosen by the manufacturer; there can be many brand names for a drug
Chapter 15- autonomic nervous system
CNS- brain & spinal cord
Peripheral Nervous system
o Somatic (voluntary)- skeletal muscle movement
o Autonomic (Involuntary)- smooth muscles and glands
Sympathetic (adrenergic) FIGHT OR FLIGHT
Dilates pupil
Inhibits saliva production
Dilates bronchi- RELAX AIRWAYS
Accelerates heart
Stimulates epinephrine & norepinephrine release
Stimulates glucose release
Inhibits stomach, pancreas, and intestines
Inhibit gall bladder
Relax bladder
Inhibits urination
Promotes ejaculation & vaginal contractions
NOREPINEPHRINE (CATECHOLAMINE) neurotransmitter
o Receptors
ALPHA 1 & 2
BETA 1 & 2
Parasympathetic (cholinergic)- REST & DIGEST
Constricts pupil
, Stimulates saliva production
Constricts bronchi
Slows heart
Stimulates stomach, pancreas, & intestines
Stimulate gall bladder
Contract bladder
Stimulates urination
Promotes erection of genitals
ACETYLCHOLINE (neurotransmitter)
o Receptors
NICOTINIC- neuromusclular; affects skeletal muscles
MUSCARINIC- stimulates smooth muscle; slows heart rate
Adrenergic Antagonist: mimic parasympathetic by blocking access to the adrenergic receptor sites
o Adrenergic blockers
o Sympatholytic
o Rest & digest
o Beta blocker- specifically block beta receptor sites & inhibit norepinephrine and epinephrine
Decrease BP & HR
Cause bronchoconstriction
End in -LOL
o Alpha Adrenergic blockers- inhibit release of epinephrine
End in -ZOSIN
o Bronchospasm
o Metoprolol Advers
o Labetalol
o e
Atenolol: treat HTN, migraine prophylaxis, angina, MI, HF (Side effects: depression, sexual dysfunction,
cool extremities, bronchoconstriction
rxna
Adrenergic Agonist: mimic sympathetic
drenerg
o Adrenergics
ic
o Sympathomimetic- mimic the sympathetic neurotransmitters norepinephrine & epinephrine
o Fight or flight antago
o Increased heart rate
o Increased blood sugar nist
o Vasoconstriction effects
Adverse rxnadrenergic effects
o Albuterol- treats bronchoconstriction
o Epinephrine- treats allergy, anaphylaxis, asthma, cardiac arrest, severe hypotension
Patient has a cold and wonders if OTC medications are okay. You know that many of the products contain
sympathomimetics. Your patient is currently being treated for HTN. What do you tell her?
o Advise patient to consult PCP as OTC meds may elevate her already high blood pressure and increase
heart rate putting her at risk for hemorrhagic stroke.
You have been asked to administer metoprolol to a hospitalized patient. Which 2 vital signs will you check?
o Heartrate
o BP
Chapter 16
Cholinergic Agonists
Chapter 2
Agonists- drugs that produce a response
o Ex) Beta adrenergic agonist: epinephrine
Antagonists- drugs that prevent or block a response
o Ex) Beta adrenergic blocker: metoprolol
Half-life- the time it takes for one half of a drug concentration to be eliminated from the body
Therapeutic Index (Window)- the level of the drug between the minimum trough concentration in the plasm a
for obtaining desired drug action and the minimum peak concentration
o Peak- the point at which plasma drug levels are the HIGHEST
o Trough- the point at which plasma drug levels are the LOWEST
Loading dose- given to achieve a rapid concentration
A patient on two highly protein-bound drugs is at risk for accumulation of one or both drugs and toxicity.
Tolerance- a decreased responsiveness over the course of therapy which may lead to the need to increase
dosages to attain the same effect
Drugs in the same class share many common features, it is extremely helpful to learn drugs by their
classifications
Drugs can be in a class with other drugs because…
o The drugs are related by their chemical structure
o The drugs work in the same way
o The drugs are used for the same purpose
Pharmaceutic Stage: ONLY TABLETS & CAPSULES GIVEN PO
o This is the process by which the tablet/capsule becomes a solution to pass the membrane of the
stomach or small intestines
Pharmacokinetic Phase: the process of drug MOVEMENT through the body to achieve drug action
o Absorption: movement of the drug into the bloodstream after administration
Most oral drugs are absorbed through the action of mucosal villi in the small intestines
Fat-soluble (lipid soluble) & Non-Ionized drugs are MOST EASILY absorbed by the GI tract
PARENTERAL DRUGS DO NOT PASS THROUGH THE GI TRACT
o Distribution- the process by which the drug becomes available to body fluids and body tissues from the
bloodstream
Affected by rate of blood flow, the drug’s affinity to the tissue, and protein binding
Protein binding- some drugs have a HIGH affinity for binding to the plasma proteins while others
have a LOW affinity to binding
Warfarin & furosemide HIGH
Lisinopril & metoprolol LOW
Drugs that are STUCK onto proteins AREN’T FREE to go to their target and do their job
Portion that remains FREE is the ACTIVE DRUG
2 highly protein bound drugs fight for binding sites leaving more FREE DRUGS leading to
accumulation & toxicity
Low PROTEIN (ALBUMIN) DECREASES binding sites
o Metabolism/biotransformation- the process in which the body chemically changes drugs into a form that
can be excreted
LIVER IS THE MAIN SITE OF METABOLISM
FIRST PASS EFFECT-also called hepatic 1st pass
Drugs are altered by passing through the intestinal lumen into the portal vein into the
liver
This is the reason some drugs CANNOT be given PO
, Bioavailability- the % of the administered dose that reaches systemic circulation (%
available for activity)
HALF-LIFE- the time it takes for the amount of drug to be reduced by ½
Affected by the amount of drug administered, the amount of drug remaining,
metabolism, & elimination
DRUGS WITH A ½ LIFE >24H SHOULD NOT BE GIVEN MORE THAN BID (DIGOXIN &
COUMADIN)
o Excretion/Elimination- process by which the drug is excreted
Kidneys, lungs, bile, saliva, sweat, breast milk
o Pharmacodynamics- onset, peak and duration of action
Onset- the time until minimum effective action/concentration
Peak- when the drug reaches its HIGHEST blood concentration
Duration of action- the length of time the drug produces a therapeutic or pharmacologic effect
o 7 MECHANISMS OF ACTION
Stimulation- fight or flight responseadrenergic drugs
Depression- decrease neural activityseizure & pain drugs
Irritation- noxious effectastringents
Replacement- replace body compoundsinsulins and hormones
Cytotoxic action- kill invading cancers or parasiteschemo
Antimicrobial action- prevent, inhibit, kill infectious organismsantibiotics
Modification of immune status- modify, enhance, depress immune systemmethotrexate
o Drug Names
Generic- chosen by a variety of official bodies
Usually are r/t the chemical components of the drug
Brand- chosen by the manufacturer; there can be many brand names for a drug
Chapter 15- autonomic nervous system
CNS- brain & spinal cord
Peripheral Nervous system
o Somatic (voluntary)- skeletal muscle movement
o Autonomic (Involuntary)- smooth muscles and glands
Sympathetic (adrenergic) FIGHT OR FLIGHT
Dilates pupil
Inhibits saliva production
Dilates bronchi- RELAX AIRWAYS
Accelerates heart
Stimulates epinephrine & norepinephrine release
Stimulates glucose release
Inhibits stomach, pancreas, and intestines
Inhibit gall bladder
Relax bladder
Inhibits urination
Promotes ejaculation & vaginal contractions
NOREPINEPHRINE (CATECHOLAMINE) neurotransmitter
o Receptors
ALPHA 1 & 2
BETA 1 & 2
Parasympathetic (cholinergic)- REST & DIGEST
Constricts pupil
, Stimulates saliva production
Constricts bronchi
Slows heart
Stimulates stomach, pancreas, & intestines
Stimulate gall bladder
Contract bladder
Stimulates urination
Promotes erection of genitals
ACETYLCHOLINE (neurotransmitter)
o Receptors
NICOTINIC- neuromusclular; affects skeletal muscles
MUSCARINIC- stimulates smooth muscle; slows heart rate
Adrenergic Antagonist: mimic parasympathetic by blocking access to the adrenergic receptor sites
o Adrenergic blockers
o Sympatholytic
o Rest & digest
o Beta blocker- specifically block beta receptor sites & inhibit norepinephrine and epinephrine
Decrease BP & HR
Cause bronchoconstriction
End in -LOL
o Alpha Adrenergic blockers- inhibit release of epinephrine
End in -ZOSIN
o Bronchospasm
o Metoprolol Advers
o Labetalol
o e
Atenolol: treat HTN, migraine prophylaxis, angina, MI, HF (Side effects: depression, sexual dysfunction,
cool extremities, bronchoconstriction
rxna
Adrenergic Agonist: mimic sympathetic
drenerg
o Adrenergics
ic
o Sympathomimetic- mimic the sympathetic neurotransmitters norepinephrine & epinephrine
o Fight or flight antago
o Increased heart rate
o Increased blood sugar nist
o Vasoconstriction effects
Adverse rxnadrenergic effects
o Albuterol- treats bronchoconstriction
o Epinephrine- treats allergy, anaphylaxis, asthma, cardiac arrest, severe hypotension
Patient has a cold and wonders if OTC medications are okay. You know that many of the products contain
sympathomimetics. Your patient is currently being treated for HTN. What do you tell her?
o Advise patient to consult PCP as OTC meds may elevate her already high blood pressure and increase
heart rate putting her at risk for hemorrhagic stroke.
You have been asked to administer metoprolol to a hospitalized patient. Which 2 vital signs will you check?
o Heartrate
o BP
Chapter 16
Cholinergic Agonists