Pharm Final PPT Review Flashcards
What is pharmacology?
The study of drugs and their effects on living organisms.
Define toxicology.
The study of the adverse effects of chemicals on living organisms.
What are agonists?
Substances that activate receptors to produce a biological response.
What are antagonists?
Substances that block or inhibit the action of agonists at receptors.
Differentiate between competitive and non-competitive antagonists.
Competitive antagonists bind reversibly to the same site as agonists; non-competitive antagonists bind to a different site.
What does pharmacodynamics study?
The effects of drugs on the body and their mechanisms of action.
What does pharmacokinetics study?
The absorption, distribution, metabolism, and elimination of drugs.
What is pharmacogenomics?
The study of how genes affect a person’s response to drugs.
Define ‘receptor’ in pharmacology.
A protein molecule that receives and transmits signals in response to drug binding.
What is the difference between endogenous and exogenous substances?
Endogenous substances are produced within the body; exogenous substances come from outside the body.
What are poisons?
Substances that can cause harm or death when introduced into the body.
Can be organic or inorganic
What are toxins?
Poisonous substances produced by living organisms.
Define ‘partial agonist.’
A substance that activates a receptor but produces a less than maximal response.
In the presence of a full agonist, it can act like an antagonist
What is an inverse agonist?
A substance that binds to a receptor and induces the opposite effect of an agonist. This effect can bring the response lower than the constituent level of activity.
What is stereoisomerism?
The existence of molecules with the same molecular formula but different spatial arrangements.
What is a physiologic antagonist?
A substance that counteracts the effects of another substance through different mechanisms.
What does the acronym ADME stand for in pharmacokinetics?
Absorption
Distribution
Metabolism
Elimination
What is the Henderson-Hasselbalch equation used for?
To calculate the pH of a solution based on the concentrations of acid and base. Remember, if pH<pka, the compound will be in its protonated form. If pH>pka, it will be unprotonated.
Protonated acidic drugs will be neutral and more likely cross barriers, while protonated basic drugs will have a positive charge and be less likely to cross barriers.
If pH < pKa, what form is favored?
The protonated form.
Protonated acidic drugs will be neutral and more likely cross barriers, while protonated basic drugs will have a positive charge and be less likely to cross barriers.
If pH > pKa, what form is favored?
The unprotonated form.
Unprotonated acidic drugs will be negatively charged and less likely to cross barriers, while unprotonated basic drugs will have a neutral charge and be more likely to cross barriers.
What is a dose-response curve?
A graph that shows the relationship between drug dose and the magnitude of response.
What is rational dosing?
The goal to achieve the desired beneficial effect with minimal adverse effects.
What does the term ‘volume of distribution’ refer to?
A pharmacokinetic parameter that describes the distribution of a drug throughout the body’s fluids and tissues.
Higher Vd means that the drug is more likely to leave the vascular space and settle into tissues
What is clearance in pharmacokinetics?
The rate at which a drug is removed from the body.
What is meant by ‘first order’ and ‘zero order’ elimination?
‘First order’ means the rate of elimination is proportional to the drug concentration; ‘zero order’ means the rate is constant regardless of concentration.
What is half-life?
The time required for the concentration of a drug in the blood to decrease by half.
What factors affect passive diffusion?
Molecular weight
pKa
Lipid solubility
Plasma protein binding
What are the four basic mechanisms of transmembrane signaling?
- Direct crossing to intercellular receptor
- Enzymatic action mediated by ligand binding
- Tyrosine kinase activated receptors
- G protein-coupled receptors*
What is the function of ligand-gated ion channels?
To open or close in response to the binding of a ligand, allowing ions to flow across the membrane.
What is the structure of GPCR?
Comprised of seven trans-membrane alpha-helices.
What is pleiotropy in pharmacology?
The ability of a drug to produce multiple effects through different mechanisms.
What are drug efflux transporters?
Proteins that transport drugs out of cells, often involved in multi-drug resistance.
What is the blood-brain barrier?
A selective permeability barrier that protects the brain from harmful substances.
What is biotransformation?
The process by which the body chemically alters a drug.
What are the two phases of biotransformation?
Phase I: Oxidation, Reduction, Hydrolysis
Phase II: Conjugation
What does cytochrome P450 do?
It is a family of enzymes involved in the metabolism of drugs.
What is the effect of P450 induction?
Increased metabolism of drugs, which can lead to decreased drug effects.
What is the effect of P450 inhibition?
Decreased metabolism of drugs, which can lead to increased drug effects.
What is the enteric nervous system?
The nervous system of the gastrointestinal tract.
What are the classes of neurotransmitters?
Esters
Monoamines
Amino Acids
Purines
Peptides
Inorganic gases
What is the primary action of sympathetic activity on the heart?
Accelerates heart rate via β1 and β2 receptors.
What is the primary action of parasympathetic activity on the heart?
Decelerates heart rate via M2 receptors.
What is the effect of alpha-1 receptor activation?
Smooth muscle contraction.
What is the mechanism of action of adrenergic agonists?
Stimulate adrenergic receptors to produce effects like increased heart rate and vasodilation.
What are direct-acting adrenergic agonists?
Albuterol
Clonidine
Dobutamine
Dopamine
Epinephrine
Isoproterenol
Norepinephrine
What are indirect-acting adrenergic agonists?
Amphetamine
What is a key characteristic of beta-blockers?
They decrease heart rate and cardiac output.
What is the action of nitrates on vascular smooth muscle?
They relax vascular smooth muscle by increasing cGMP.
What is the difference between dihydropyridines and non-dihydropyridines in calcium channel blockers?
Dihydropyridines are more selective for peripheral vasculature; non-dihydropyridines affect the heart more.
What does SLUDGE-M stand for in toxicology?
Salivation
Lacrimation
Urination
Diarrhea
Gastrointestinal distress
Emesis
Miosis
What is the primary treatment for organophosphate poisoning?
Atropine and Pralidoxime.
What is the action of cholinomimetics?
They mimic the action of acetylcholine.
What is a common side effect of cholinomimetics?
Bradycardia.
What is the primary therapeutic use of cholinomimetics?
Treating conditions like myasthenia gravis.
What is an adrenoceptor antagonist?
A substance that blocks the action of catecholamines at adrenoceptors
Examples include propranolol, which antagonizes β1 & β2 receptors.
What is the primary action of Propranolol?
Lowers blood pressure and prevents reflex tachycardia
It antagonizes β1 & β2 receptors and decreases cardiac output.
Name three α1 blockers.
- Prazosin
- Terazosin
- Doxazosin
What do α1 blockers do?
Block α1 receptors in arterioles and venules, leading to vasodilation.
What is the mechanism of Minoxidil?
Opens K+ channels in smooth muscles, stabilizing potential and reducing contraction.
What does Hydralazine do?
Dilates arterioles through nitric oxide production.
What is the toxicity associated with vasodilators?
Headache, nausea, sweating, flushing.
What is Sodium Nitroprusside used for?
Hypertensive emergencies and cardiac failure.
What is the mechanism of action of Sodium Nitroprusside?
Relaxes vascular smooth muscle by breaking down in blood to release NO.
What is Captopril?
An ACE inhibitor used to treat heart failure.
What are the two types of heart failure?
- Systolic failure – reduced cardiac function
- Diastolic failure – reduced cardiac filling
What is the consequence of congestive heart failure?
Increased left ventricle pressure at end diastole leading to pulmonary edema.
What are the four factors that affect cardiac performance?
- Preload
- Afterload
- Contractility
- Heart Rate
What does Digoxin do?
Inhibits Na+/K+ ATPase, maintaining normal resting potential and acting as a positive inotrope.
What is the therapeutic range for Digoxin toxicity?
EC50 – 1 ng/mL, TC50 – 2 ng/mL.
What are phosphodiesterase inhibitors known for?
Inactivating cAMP and cGMP, providing positive inotropic effects.
What is the sinoatrial node?
The pacemaker of the heart located in the right atrium.
What is required for reentry in cardiac impulse conduction?
- An obstacle (scar tissue)
- Unidirectional block
- Long enough conduction time
List the four classes of antiarrhythmic agents.
- Class I – sodium channel blockade
- Class II – sympatholytic
- Class III – prolong action potential duration
- Class IV – block cardiac calcium channel currents
What is Amiodarone known for?
The only antiarrhythmic with all four Vaughan-Williams’ class effects.
What is the first-line treatment for bradycardia?
Atropine.
What are the effects of H1 receptors?
- Bronchoconstriction
- Vasodilation
What is Diphenhydramine used for?
Type I hypersensitivity reactions.
What do leukotrienes do?
Cause bronchospasm, mucous secretion, and airway edema.
What is the action of Montelukast?
Inhibits binding of leukotrienes to their receptors.
What is the role of Omalizumab?
An anti-IgE monoclonal antibody that reduces asthma severity.
What is serotonin syndrome?
A potentially life-threatening condition caused by excessive serotonergic activity.
Name the three major classes of antidepressant medications.
- Monoamine oxidase inhibitors (MAOIs)
- Tricyclic antidepressants (TCAs)
- Selective serotonin reuptake inhibitors (SSRIs)
What is the therapeutic range for phenytoin?
10-20 mcg/ml for therapeutic, >30 mcg/ml for toxic.
What is the main effect of benzodiazepines in seizure treatment?
Sedation.
What is the therapeutic plasma level range for phenytoin?
10-20 mcg/ml
Free phenytoin levels range from 1-2.5 mcg/ml.
What are the toxic and lethal plasma levels for phenytoin?
Toxic: 30-50 mcg/ml; Lethal: >100 mcg/ml
What should be the next option for a status epilepticus patient not responding to Phenytoin or phenobarbital?
Benzodiazepines, consider intubation
Why are second generation antihistamines preferred over first generation in allergy symptom relief?
They do not cause sedation
Which of the following is a selective serotonin reuptake inhibitor?
Sertraline (Zoloft)
What are the phases of platelet activity in thrombogenesis?
- Adhesion
- Aggregation
- Secretion
- Cross-linking of adjacent platelets
What are the intrinsic and extrinsic pathways of blood coagulation?
Intrinsic: Collagen, vWF; Extrinsic: TF
What is the treatment for disseminated intravascular coagulation (DIC)?
- Plasma transfusions
- Treat underlying cause