Exam 1 Flashcards
Definition of Pharmacology
Study of introducing chemical agent into a living system (Origin, Chemistry & Effects of a drug)
Definition of Pharmacodynamics
Effects of drug on living system
Definition ofPharmacokinetics
How the body response to a drug (4 aspects)
1) Absorption
2) Distribution
3) metabolism
4) Elimination
Definition of Prodrug
Drug that’s INACTIVE when you take it
B1 is in the…
Heart
B2 is in the…
Non vascular smooth muscle (causes it to relax)
Definition of Pharmacotherapeutics
Use of drugs to Dx, Tx or prevent disease
Definition of Toxicology
Study of Poisons
Definition of Pharmacognosy
Study of drugs in crude form (original source/plant-based)
Definition of Drug vs. Medication
Drug: ONE chemical agent
Med: ONE OR MORE chemical agents
Definition of Synergism
1+1=21 (sum of 2 or more agents is greater than sum of individual effects) “enhancing”
Definition of Antagonism
Blocks effect of agonist
Example of Antagonism
Naloxone Tx for Heroin overdose
Definition of Hypperactivity
Response greater than anticipated to a given dose
Definition of Tolerance
Prolapsed exposure to liver causes enzyme induction (liver increases enzyme to inactivate the drug)
Definition of Tachyphylaxis
Form of tolerance that only occurs after 2-3 doses
Definition of Adverse reaction
Reaction that warrants DC of the drug
Definition of Habituation
Psychological Dependance
Definition of Addiction
Physical Dependance
Definition of Bioavailability
What % of dose really makes it to the target tissue
Definition of First-Pass Effect
Effect the liver, stomach, intestines has on drug
Liver is MC to break down
What is the most effective way to deliver a drug?
IV so it bypasses the Liver
Definition of Proprietary
Owns the Name of the Drug (BRAND NAME)
(ADVIL)
Definition of Non-Proprietary
Same drug but under a different name (WALGREEN”S BRAND)
Patient-Related Factors that influence Drug Safety & Effectiveness (10)
1) Weight (mg/kg)
2) Age (young & old)
3) Sex
4) Physiological
5) Pathological
6) Nutrition
7) Allergy-Hypersensitivity Reaction
8) Enzyme Induction
9) Hormonal Factors
10) Pt. Compliance
Definition of Dyscrasias
Abnormal Blood Work
Do side effects affect Compliance?
YES
What are Concomitant drugs?
Taking 2 or more drugs at the same time
Most Thearapeutic bonds are…
IONIC
What are ionic therapeutic bonds?
Weak, easily digested, used and excreted
What is a covalent therapeutic bond?
IRREVERSIBLE/not wanted
Indy’s to heavy metals and pulls it out of the tissue
What type of curve is the Dose-Response Curve?
Logarithmic Curve
Definition of Potency
How much your taking (DOSE)
Definition of Slope
Steeper the slope, less of the drug you have to take to get the same effect
Definition of Maximal efficacy
Effect (variability)
Definition of Median Effective Dose (ED50)
Dose at which 50% of population will get the maximum effect
Definition of Median Lethal dose (LD50)
Dose at which 50% of population will die if they take that dose
Definition of Theurpeutic Index
[LD50 / ED50]
Higher TI -> less likely to kill you
Example of Competitive drug
Atropine for nerve gas
MC route for absorption
Simple Passive diffusion
MC route for absorption in GI tract
ORAL (1st order kinetics)
Inhalation is the…
2nd Most Effective way to absorb (B2 receptors)
Parenteral Administration most effective route
IV
Definition of Zero-Order Kinetics
Drug absorbption that proceeds at a constant rate
(Can give all @ once or push w/ an IV)
Definition of First-Order Kinetics
Absorption that proceeds @ a changing rate but is always proportional to the amount absorbed (take 500mg and after 1 hour have 250mg left)
Definition of Drug Metabolism
Converting pharmacologically inactive drug into metabolites
Example of a Prodrug
Theophylline for Asthma
Definition of Phase I of Biotransformation
Inactivation of a drug to diminish its overall effect
Example of Phase I Biotransformation
1) Hydrolysis
2) Oxidation
3) Reduction
Definition of Phase II Biotransformation
To convert lipid sable into water soluble
Examples of Phase II Biotransformation
1) Glucuronide Formation
2) Acetylation
3) Sulfate Conjugation
4) Methylation
Example of Glucunoride Formation
Unconjugated Bilirubin -> Glucunoride Formation -> H20 soluble (Conjugated)
Major pathway of drug excretion:
Renal Excretion
2nd MC pathway of Excretion:
Biliary Excretion
Oral Meds are what order kinetics?
1st
IV Meds are what order kinetics?
Zero
What does Elixir mean?
Med has a % of alcohol in it
1 teaspoon =
5mL or 5 cc’s
1 Tablespoon =
3 teaspoons, 15mL or 15 cc’s
1 ounce =
2 Tablespoons, 6 teaspoons or 30 cc’s
3 major functions of the Autonomic NS
1) heart
2) Secratory function
3) contraction/Relaxation of Smooth muscle
3 Major elements of the Autonomic NS
1) Afferent Limb
2) Central Intergrated Elements
3) Efferent Limb
What does the Afferent limb of the Autonomic NS do?
Carries sensory from peripheral to spinal cord (GVA)
What does the Central Integrated Element of the Autonomic NS do?
Info is processed to Hypothalamus/Lower brain
What does the Efferent limb of the Autonomic NS do?
Carrie motor to neuroeffector tissues (GVE)
What receptors are located in the Parasympathetic NS?
ALL Cholinergic (ACh)
What receptors are located in the Sympathetic NS?
Mostly Noradrenergic (norepinephrine)
Parasympathetic vs. Sympathetic Effects on the Heart:
P: Slow down
S: Speed up
Parasympathetic vs. Sympathetic Effects on the Sexual Organs:
P: Arousal
S: Orgasm
Primary neurotransmitter of the Cholinergic System is _________ and it is released from the ____________.
ACh; PREsynaptic & POSTsynaptic Axon terminal
Cholinoceptors (2)
1) Muscarinic (autonomic NS)
2) Nicotinic
Edinburg Westphal Nucleus: CN & Function
3; smooth eye muscle
Superior Salivatory Nucleus: CN & Function
7; Lacrimal glands & Salivary Glands (except parotid)
Inferior Salivatory Nucleus: CN & Function
9; Parotid Gland
Dorsal Motor Nucleus of the Vagus Nerve: CN & Function
10; Thoracic & Abdominal Viscera
Basic functions of the Parasympathetic NS
1) dec. Heart rate
2) inc. GI secretions
3) miosis
4) Near vision accommodation
5) defecation
6) Emptying Bladder
7) Bronchial smooth Muscle contraction
Enzyme for ACh:
Acetylcholinesterase
Type 2 Nicotinic receptors are located
In all autonomic NS ganglia & the Adrenal Medulla
Stimulation of Type 2 Nicotinic receptors results in the release of…
1) ACh (parasympathetic)
2) norepinephrine (sympathetic)
3) epinephrine (adrenal medulla)
Type 1 Nicotinic receptors are located
At NMJ of somatic muscles
Function of Type 1 Nicotinic receptors
Skeletal Muscle Contraction
Muscarinic Receptors are located in
All parasympathetic target organs
Function of Muscarinic Receptors
1) Near vision (ciliary muscles)
2) Miosis (iris sphincter
3) Dec. heart rate
4) contract Bronchi
5) GI secretion
6) Sweating
7) Penile erection
8) Vasodilation
2 sites where drugs can act in the autonomic NS
1) Synapse between Pre & Post ganglionic neurons
2) Junctions between post ganglionic & effector organ
Definition of Direct Stimulation Neurotransmitter
Drugs mimic same effect as ACh or Norepinephrine
Definition of Indirect Neurotransmitter Stimulation
Drugs given that inactivate an enzyme (ACh-nerve gas)
Definition of Block Receptor Neurotransmitter
Drugs that compete for same receptor site
Lytic means:
Blocking the effect
Origin & where they exit (Preganglionic neurons in the Sympathetic NS)
Lateral horn of Thoracolumbar spinal cord (T1-L2)
GVE fibers exit through ventral Root via white rami
White Rami ______ and Gray Rami ________
Exit SC; Enter SC
Basic function of sympathetic NS
1) inc. heart rate & force
2) BronchoDilation
3) Mydriasis
4) Sweating
5) Smooth muscle of blood vessels
6) Dec. GI motility
Adrenergic neurotransmitters that affect the Somatic NS
[Synthesized from Tyrosine]
- Norepinephrine
- epinephrine
- amino acids
Receptors of the Sympathetic NS:
Cholinergic
Norepinephrine is released from
POSTganglionic axons of Adrenal Medulla
Epinephrine is released from:
Adrenal Medulla
Norepinephrine and Epinephrine are broken down by:
80% is re-uptake into PREsynaptic neuron terminus
Norepinephrine and Epinephrine are inactivated by __________ in the Neuron Terminus.
MAO (MonoAmine Oxidase)
Norepinephrine and Epinephrine that are left in the Synaptic Cleft are inactivated by
COMT (Catechol-O-Methyl Transferase)
Alpha-1 Sympathetic are what type of Receptorr?
Adrenergic
Alpha-1 Receptor Bodily Reactions
Eye: contract radial muscles or iris
Arterioles: Constrict
Veins: Constrict
Sex Organs: Ejaculation
Bladder, Neck & Prostate: Constrict
Alpha 2 Receptor Site
PREsynaptic nerve terminal
Alpha 2 Function
Inhibit Neurotransmitter release
Beta 1 Bodily Reactions
Heart: inc. rate, force & AV conduction velocity
Kidney: Release Renin
Beta 2 Bodily Reactions
Arterioles: Dilation, heart, lungs, skeletal muscle
Bronchi: Dilation
Uterus: Relaxation
Liver: Glycogenolysis
Dopamine Effect on Kidney:
Dilation of Renal Vasculature
5 Neurotransmitters that bind to Autonomic Receptors:
1) Nitric Oxide
2) GABA
3) ATP
4) Neuropeptide Y
5) Vasoactive Intestinal peptide (VIP)
Main pharmacological Target organs in Clinical Medicine are…
- Gut
- Heart
- Lungs
- Blood Vessels
Sympathetic Muscarinic Receptors are located on:
- Eccrine Sweat Glands
- Blood vessels in Skeletal Muscle
Sympathetic Nicotinic Receptors are located on:
- Cells of Adrenal Medulla
- POSTganglionic neuron cell bodies & Dendrites
3 ways to Manipulate the Adrenergic System using Sympathomimetic-Adrenomimetic processes:
1) Sympathomimetic drugs as agonists (direct)
2) Inhibit uptake (Indirect)
3) Inhibit MAO (Indirect)
3 ways to Manipulate the Adrenergic System using Sympatholytic processes:
1) Dec. Norepinephrine Release
2) Block Adrenergic Recpetors (Alpha/Beta Blockers)
3) Stimulating Alpha 2 Receptors
Definition of Cholinomimetic:
Mimic the effect of ACh
Cholinomimetic Muscarinic Agonists (3) Examples
Bethenechol
Pilocarpine
Muscarine
Bethanechol is used for
- Relieving Constipation
- Paralytic Ileus
- Urinary Retention
Pilocarpine is used for:
- Treating Glaucoma
- Increase Aqueous Outflow
Muscarine is gathered from
Certain toxic Mushrooms
Adverse effects of Direct Acting Cholinomimetic’s
- Diaphoresis
- hypotension/bradycardia
- inc. salivation & gastric acid
- abdominal cramps & diarrhea
- exacerbation of asthma
Reversible Cholinesterase Inhibitors (Indirect Acting Cholinomimetic’s)
- Neostigmine
- Physostigmine
- Edrophonium
Neostigmine is used for
Treating Myasthenia Gravis
Physostigmine is used as a
Cholinergic agent
Edrophonium is used for
Diagnosing Myasthenia Gravis
Adverse Effects of Indirect Acting Cholinomimetic’s
- Miosis/blurred vision
- inc. salvation, lacrimation, GI & respiratory secretions
- abdominal cramps & diarrhea
- diaphoresis
- bradycardia
- neuromuscular blockade & paralysis
Muscarinic Antagonists are found in
Smooth Muscle & Cardiac Muscle
Function of Atropine
Blocks Muscarinic Receptors (ANTAGONIST)
Where is Atropine located?
POSTganglionic & POSTsynaptic site
Bodily Reactions from Atropine:
- inc. heart rate
- mydriasis
- Dec. secretions
- Dec. tone of urinary and respiratory tracts
Higher doses of Atropine can cause
Hallucinations & Delirium
Parasympatholytic Muscarinic Antagonist: (e.g.)
Atropine
Adverse Effects of Muscarinic Antagonists:
- Xerostomia
- Blurred Vision/Photophobia
- inc. Intraocular pressure
- urinary retention
- constipation
- anhydrosis
- tachycardia
- exacerbates asthma
Definition of Adrenomimetic Drugs
Mimic effects of norepinephrine or epinephrine
Amphetamines inhibit the re-uptake of
norepinephrine (cocaine, adderall)
Tricyclic Antidepressants inhibit
MAO
Indirect Acting Adrenomimetic Drugs promote the release of
Norepinephrine; Ephedrine
What is the MC cause of drug induced psychosis
Methamphetamine
What does methamphetamine do to the body?
1) promotes adrenergic release
2) creates hyper adrenergic state
Direct Acting Adrenomimetic Alpha 1 Agonists
Phenylephrine & Epinephrine
Direct Acting Adrenomimetic Alpha 1 Agonists Functions
Vasoconstrict & Dilate pupil
Direct Acting Adrenomimetic Alpha 1 Agonists Therapeutic Uses:
- Homeostasis
- Nasal Decongestion
- local anesthetic
- elevate BP
- Dilate Pupil (Mydriatics)
Direct Acting Adrenomimetic Alpha 1 Agonists Adverse Effects:
- Hypertention
- Localized necrosis
- Reflex Braycardia
- urinary retention in BPH patients
Direct Acting Adrenomimetic Beta 1 Agonists
Isoproterenol & Epinephrine
Direct Acting Adrenomimetic Beta 1 Agonists Therapeutic Uses:
Cardiac Arrest (initiate contraction)
Shock (positive ianotropic and chronotropic effects)
Direct Acting Adrenomimetic Beta 1 Agonists Adverse effects
Angina pectoris & Tachycardia
Direct Acting Adrenomimetic Beta 2 Agonists
Isoproterenol, Epinephrine & Terbutaline
Direct Acting Adrenomimetic Beta 2 Agonists Therapeutic uses
Asthma: Bronchodilator
Delay Preterm labor (Relaxes Uterus)
Direct Acting Adrenomimetic Beta 2 Agonists Adverse effects
Hyperglycemia
Direct Acting Adrenomimetic Multiple Receptor Activation is Used for
Tx of Anaphalactic Shock
Problems with Direct Acting Adrenomimetic Multiple Receptor Activation
- Hypotension
- Glottis Edema
- Bronchoconstriction
Indirect Acting Adrenomimetic Drugs
Tricyclic Antidepressants, MAO inhibitors & Ephedrine
What is special about Ephedrine?
It’s a mixed-acting agent causing Norepinephrine release and activation of alpha and beta receptors directly
Indirect Acting Adrenomimetic Drugs Therapeutic Uses
- Nasal Congestion
- Asthma
- Narcolepsy
Indirect Acting Adrenomimetic Drugs Adverse Effects
Hypertension & Angina
Alpha 1 Adrenergic Antagonists:
Prazosin
Phentolamine
Phenoxybenzamine
Alpha 1 Adrenergic Antagonists Function
Vasodilation
Alpha 1 Adrenergic Antagonists Therapeutic uses:
- Essential Hypertension
- Benign Prostatic Hyperplasia (Dec. Smooth muscle tone)
- Pheochromocytoma
Alpha 1 Adrenergic Antagonists Adverse effects
- Orthostatic hypertension
- Reflex tachycardia
- Nasal congestion
- Inhibition of ejaculation
Beta 1 Adrenergic Antagonists:
Propranolol (Inderal)
Metoprolol (Lopressor)
Tim o lol
Beta 1 Adrenergic Antagonists Bodily Reactions
- Dec. heart rate & force
- dec. conduction velocity
Beta 1 Adrenergic Antagonists Therapeutic uses
- hypertention
- angina pectoris
- hyperthyroidism
- stage fright
- glaucoma
- migraine’s
Beta Adrenergic Receptor Antagonists Adverse Reactions
- bradycardia
- Dec. cardiac output
- bronchoconstriction
- insomnia
- depression
- Dec. libido
Botulism Toxin prevents release of
ACh
Nicotine promote release of
Neurotransmitters from POSTganglionic neurons
Ephedrine, Amphetamines and Tyramine promote release of
Norepinephrine
AChase is inhibited by
Physostigmine
Organophosphate
Carbamates
Clonidine is a __________ antagonist used to treat ______________.
Alpha 2; Hypertension
MC Neurotransmitter in the CNS & PNS
Norepinephrine
Excitatory vs. Inhibitory: Norepinephrine
Excitatory
Excitatory vs. Inhibitory: Serotonin
Excitatory
Excitatory vs. Inhibitory: Dopamine
Inhibitory
Excitatory vs. Inhibitory: GABA
Inhibitory to the CNS
What processes are Affected by: Norepinephrine
- Sleep/Wake
- Learning & Memory
- Mood
What processes are Affected by: Serotonin
- Sleep/Wake
- Pain perception
- depression
- Sexual Activity
- Aggressive Behavior
Dopamine Is found in:
Substantial Nigra
Caudate Nucleus
Serotonin Is found in:
Hypothalamus
Limbic System
Brain Stem
Norepinephrine Is found in:
Pons
Neurons of Reticular Formation
What neurotransmitters are derived from Tyrosine?
Norepinephrine
Dopamine
What neurotransmitter is derived from Tryptophan?
Serotonin
What does GABA do to the nerve?
Enhances Cl- ions; decreasing Firing
Excitatory vs. Inhibitory: Glycine
Inhibitory
Excitatory vs. inhibitory: Glutamine Acid
Excitatory (classified as a stimulant))
3 things that exaggerate neurotransmitter effect by increasing the neurotransmitter at the synapse
1) Inc. rate of synthesis & release (amphetamines)
2) Dec. enzyme breakdown (cocaine)
3) Prolong the time in the synapse (atropine)
4 things that decrease the overall effect of a neurotransmitter
1) Dec. synthesis or release
2) inc. rate of enzyme breakdown
3) inc. pre-synaptic uptake
4) block post-synaptic receptor sites
Analeptic Stimulants: MOA
Inhibits GABA
Analeptic Stimulants: Example
Doxapram
Analeptic Stimulants: Clinical Use
- Doxopram stimulates respiration in pt’s w/ barbiturate overdose
- Post-anesthetic pt’s
- Neonatal RDS
Psychomotor Stimulants: MOA
Inc. norepinephrine release from pre-synaptic neurons
Psychomotor Stimulants: Examples
Methylphenidate (Ritalin)
Adderall
Psychomotor Stimulants: Clinical Use
Hyperkinesis (ADD)
Obesity
Narcolepsy
Psychomotor Stimulants: Acute Effects
Euphoria
Dizziness
Tremor
Irritability
Insomnia
Tachycardia
Arrhythmias
Methylxanthines: MOA
Dec. chloride conductance
Dec. adenosine activity at post-synaptic sites
Methylxanthines: Examples
Caffeine
Methylxanthines: Clinical use
BronchoDilation
Tx of CNS depressant overdose
Fatigue
Headaches
Endogenous Definition
Struggle to get out of bed in the morning even though things in your life are perfect
Exogenous definition
You had a bad weekend and are depressed
Example’s of SSRI’s
Fluoxetine (Prozac) 1/2 life = 24 hours
SSRI’s: MOA
Block re-uptake of serotonin
SSRI’s Clinical Indications/Usage
Treats OCD & Clinical Depression
SSRI’s: Side Effects
- Nausea
- Weight loss/Decreased Appetite
- Serotonin Syndrome: Jitters, Elevated core temp
Tricyclics: Examples
Amitriptyline (Elavil) - Prototype
**Prodrug (inactive when taken)
1st drug to be approved for children
Imipramine
Tricyclics: MOA
Block re-uptake of Norepinephrine, increasing levels of norepinephrine
Tricyclics: Clinical Use
Clinical Depression
Tricyclics: Adverse Reactions
Sedation, Dry-Mouth
Weight gain
Suicidal ideation
MonoAmine Oxidase Inhibitors: Examples
[Dangerous-use as last resort]
Phenelzine (Nardil)
MonoAmine Oxidase Inhibitors: MOA
Blocks enzymatic breakdown of norepinephrine in the BRAIN (90%) & Gut (10%)
W/O MAO -> Hypertensive crisis
MonoAmine Oxidase Inhibitors: Clinical Use
Clinical Depression
MonoAmine Oxidase Inhibitors: Side Effects
Have to be on Tyramine diet or else Hypertensive Crisis
Bupropion effect on the body
Suppresses Nicotine fits
Can lower seizure threshold
Anti manic Agents function
minimize the highs of a manic phase
Antimanic: examples
Lithium Salts
Antimanic Agents: MOA
Only treats manic phase; need another drug for depressive low
Anxiolytic Agents: MC Classification
Minor tranquilizers (treat psychosis)
Anxiolytic Agents: Example
Benzodiazepines (Diazepam) (Valium)
Anxiolytic Agents: MOA
Stimulates GABA (more negatively charged00
Anxiolytic Agents: Clinical Use
Anxiety
Panic Attacks
Anxiolytic Agents: Side Effects
Stronger Potency
Sedative-Hypnotic Agents: MC Classification
Insomnia
Drug therapy for Imsomnia
Benzodiazepines (taking sleeping pills ruins REM sleep causing rebound insomnia)
Sedative-Hypnotic Agents: MOA
Enhance GABA activity in the brain