Exam 1 Study Guide
Exam 1 Study Guide 4351
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This 13 page Study Guide was uploaded by Kristen Jones on Monday September 19, 2016. The Study Guide belongs to 4351 at University of Central Arkansas taught by Dr. Martin in Fall 2016. Since its upload, it has received 16 views. For similar materials see Pharmacology in Biology at University of Central Arkansas.
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Date Created: 09/19/16
Pharmakokinetics What the body does in response to a drug Pharacodynamics What the drug does to the body It all starts with administration How you give a patient a drug Enteral Administration o By way of the GI tract o Most common form is oral o Others are: Sublingual Rectal Feeding tube Parenteral Administration o By way other than the GI tract o Some include IV venous IA arterial IM muscular SQ subcutaneous (insulin for example) Other Administration o Transdermal Nicotine patch Topical creme o Inhaler Inhalation Rapid response IV, inhaler…. Both go to direct contact Benefits of oral administration o Easy o Noninvasive Downside o Takes longer to work o Takes time to absorb When rectal? o Throwing up IV benefits o Rapid results o Immediately in the blood stream Risks o Bleeding o Infection because the skin is breaking Fiving drug in target area helps to target the tissue and minimize side effects 1 you will administer an agent 2nd the drug has to be absorbed what factors influence drug absorption? o Q (blood flow) At the site of absorptions if there is not enough blood flow, there will be trouble absorbing the drug o BV Dehydration leads to a decreased blood volume which leads to a decrease in blood flow When given orally you run the risk of dehydration leading to poor absorption o Route of administration Some drug are okay to take a long time to absorb, but IV or IA is used when there is a need for rapid absorption o Solubility of the drug Lipid vs. water Lipid soluble agents cross bilayer more readily than water soluble agents because they go through the cell membranes o Degree of ionization Is it charged or uncharged Uncharged cross more readily than charged do Charged still cross, it is just more difficult If the pH is less than the pka, then the protonated form of the drug is predominant Protonated means the H form, so weak acid HA and weak base BH + HA is uncharged, BH+ is charged You would want mostly charged if you are trying to pee off or get rid of a drug, you would want uncharged if you are trying to absorb the drug Efficacy o The physiological effect on the patient o What does the drug do o What does the drug make the body do Potency o Refers to the dose of the drug that yields an effect Most drugs produce their effect by binding to specific receptors Agonists o Affinity and efficacy o Recognizes a receptor and binds to a receptor and then produces an effect Antagonists o Affinity o Will only bind to a receptor o What this drug is doing is blocking the receptors so that an agonist cannot bind to the receptor, eliminating the effect ANS- Autonomic Nervous System o Typically involuntary impulses SNS- Somatic nervous system o Voluntary motor component ANS o Heart Heart rate Contractility Influences BP and Q o Smooth Muscle Contraction Relaxation o Glands Produces secretion Increases or decreases secretion from the gland o Smooth Muscle GI smooth (digestive system) GU smooth (urinary and reproductive system) Bronchial (airways) Vascular smooth muscle o In regard to the GI and GU CTX increases activity RLX decreases activity o In regard to vascular and smooth CTX closing a tube- constriction RLX- opening a tube- dilation o Sympathetic Flight of fight Increased HR and myocardial contractility Primarily relaxes smooth muscle except vascular smooth muscle Dilates airways and pupils Decreases GI and GU activity o Parasympathetic Rest and digest decreases HR and contractility contracts smooth muscle except vascular smooth muscle stimulates gland secretion Increased GI and GU activity Constricts airways and pupils 2 different neurotransmitters o Ach Always released at all preganglionic synapses in both sympathetic and parasympathetic Always at postganglionic, sweat glands. o NE/Epi Exist in the autonomic ganglia and the synapse at the effector organ At almost all postganglionic sympathetic synapses It is Ach only at sweat glands Associated with sympathetic o Ach binds to cholinergic receptors o Epi/ NE binds to adrenergic receptors o ACH Heart Lowers HR Lowers contractility Binds to cholinergic recpetrs found in the heart GI, GU, bronchial smooth muscle Causes contraction Decreases lumen Increases activity Allows for bowel movement Bronchoconstriction Glands Stimulates production Increased secretion o Epi/NE Adrenergic receptors Sympathetic Heart Increase HR Increase contractility GI, GU, bronchial Relaxation Decreased activity Dilation Vascular Associated with blood vessels Contraction o NE/Epi o Helps to raise BP Relaxation o Epi only o Vasodilator Both can happen in flight or fight Different adrenergic receptors can be activated at the same time Some are relaxed, some are constricted to yield optimal performance for fight or flight Glands Reduce secretion when Epi/NE condition Chemicals are what produce the effects Ach cholinergic receptors o Nicotinic receptors Respond to ACH respond to nicotine Nn o Located in the autonomic ganglia o Excites the postganglionic neurons (fires) o Located in the adrenal medulla o Modified sympathetic ganglion o Increase NE/ Epi release (majorly epi) o This is the adrenaline rush Nm o Skeletal muscle o Somatic o Cell membranes o Voluntary o Effect is contraction o Binds to Nm cholinergic receptors class of drugs known as neuromuscular relaxation that targets Nm receptors that leads to relaxed paralysis o Muscarinic Responds to ACH Responds to muscarine M1 o Located on gastric parietal cells o Cells of the stomach o HCl produces stomach acid, increases HCl production, breaks down what it comes into contact with o Helps to fuel digestion M2 o Located in the heart o Reduces heart rate o Reduces contractility M3 o Located in the smooth muscle and glands o Influences contraction in regard to glands o Ach increases gland secretion Adrenergic Receptors o Alpha o Beta Activated by Epi (all types) and NE (all except for Beta 2) o Alpha A1 Vascular smooth muscle constriction increases BP Located on the presynaptic adrenergic nerve terminals (postganglionic sympathetic presynaptic nerve terminal) A2 Located on the presynaptic adrenergic nerve terminals NE release o Beta B1 Heart Increases HR Increases contractility Cardio selective- can either have an antagonist or agonist B2 All smooth muscle Increase relaxation Epi only NE EPi Alpha 1 All adrenergic receptors Alpha 2 Alpha 1 Beta 1 Alpha 2 Vascular smooth muscle Beta 1 Heart Beta 2 No NE pen because it does not Targets all receptors target bronchial Does not have B2 affinity Colinomimetics- mimics Ach Can be classified as: Indirect acting o Cholinesterase inhibitors o They do not bind to receptors o Increase the amount of ACH at a synapse o Don’t allow for metabolism to occur Direct acting o Bind to and stimulates the cholinergic receptrs o These are agonists They have affinity and efficacy o Mimic ACH Both increase ACH Both increase ACH effect Indirect acting cholinesterase inhibitors o Physostigmine and neostigmine Block degradation of ACH ultimately increase the amount of ACH available Nonselective Targets all synapses, does not select for a specific location @ skeletal muscle o spasitc paralysis o contraction and no relaxation @ heart o decrease HR o decrease CO o decrease BP @ glands o increase secretion o may be sweating more, drooling more, ect @ digestive system o increase activity o GI, GU, bronchial sm contraction is increased o Diarrhea may result What are the drugs used for? o Counter a neuromuscular blocker o Targets Nm o Blocks them o Prevents ACH from binding and causing contractions o Giving this increases ACH will compete with Nm for the binding sites o Whoever has more present wins Direct acting o Bind to and stimulate the cholinergic receptor Cholinergic Agonists: o Nicotinic Bind to nicotinic receptros o Muscarinic Bind to muscarinic receptors Bethanechol Non selective muscarinic agonist, binds to M1, M2, and M3 Where does it produce its effect? o ANS ONLY o This is where the muscarinic receptor are o No somatic effects, that is nicotinic receptors/ so more selective Parasympathetic effect on the heart: Decrease HR Sympathetic effect on the heart: Increase HR Increase contractility Anticholinergic drugs Nn o Autonomic ganglia and adrenal medulla o Ganglionic blocker (parasympathetic and sympathetic) o Trimethanphan- a lot of side effects because you are shutting down the ANS o Use trimethanphan when high blood pressure is threatening life Nm o Neuromuscular junction o Flaccid paralysis o No contraction o Uses: Anesthetic Reverse side effects of neostigmine Two examples: competitive blockers Atracurium Vecruonium Depolarizing agent Succinylcholine o Lasts about a min Muscarinic o Non-selective Will effect M1, M2, M3 o Antagonists- just bind to receptor o Atropine- sinus bradycardia o Glycopyrrolate o Ipratropium bromide What would it do? o Heart Increased HR o Bronchial smooth muscle Decrease contraction Bronchodilator o GI, GU, smooth muscle Decrease activity o True or false? Causes diarrhea? False Causes urinary retention? True Causes mucus secretion in the airways to decrease? True o Causes the side effects of o Dry mouth Decrease saliva o Blurred vision o Urinary retention o Constipation o Tachycardia Sympathomimetics Indirect aciting o Either making more NE or there is an decrease in NE reuptake o Increase in NE release Amphetamine- includes meth Tyramine- in aged cheeses, wine chocolate o Decrease reuptake Reduces or blocks reuptake Cocaine Tricyclic acid Direct acting o Act as agonists that bind to receptors Non selective Epi NE Selective Alpha 1 o Phenylephrine o Increase BP o Increases SVR o Uses as presser agent o Side effects high blood pressure o Can cause reflex bradycardia Alpha 2 o Clonidine o Functional sympatholytic o Decrease release of NE o This is an agonist Beta 1 o Agonist o Dobutamine o Increase HR o Increase contractility o Increase CO o Increase BP Positive inotrope drug that effects myocardial contractility Positive chronotrope drug that effects heart rate Beta 2 o Most commonly used to be a bronchodialotor o Rescue inhalers are an example o Terbutaline Can be given as an IV as a tocolytic agent, reduces and slows down uterine contractions and will relax smooth muscle Sympatholytics o Decrease SNS o Blockers Alpha 1 antagonist- o Lacation: vascular smooth muscles Beta 1- o Cardio selective beta blockers o Lowers HR o Lowers Contractility Beta blockers are not vasodilators
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