(no subject)
I have to go to a mandatory review tomorrow night(tonight, technically, I guess). I'm glad I know of at least one other person that will be there. I was afraid it would be me and a bunch of firefighters. Not that the firefighters in my class are bad guys or anything, I really like most of them. I just don't know them. I know I'll have someone to pal around with and gossip a little :)
The reviewing I've been doing just got a whole lot less scary, which makes me wish I'd started earlier :P You'll be happy for the cut :P
The latest gossip in the class is about some of the other young'ins. A, who recently turned into the jack ass of the class(thank goodness really, for the longest time I thought I was the only one that hated him....), and W, who is the pretty one, really, which is the only thing about her that really sticks out. She doesn't say anything of sustanence or quality, and never smiles at anyone but A. M told me that W has been spending every waking moment that she's not sleeping or working at A's office, at a private medical response company. It bothers the other employees, including M and L, who work there. The bad part is, that W will go on calls with them and everything, and start IVs and whatnot, which neither of them is ceritified to do right now, so it's very illegal and dangerous, on top of the fact that A is married, and for less than 4 months at that. A told me that they get out their books and pretend to study when anyone else walks in. No one knows if there's something between them or not, but it's fishy.
Most of the ER nurses don't even like A, lol. A's buddy D is ok, but he can be an ass too.
So that's that part. I haven't been sleeping well, but hopefully I'll go to bed soon and start on this again tomorrow. Hopefully the retest won't be too soon either. :P
I want my break to start, but I haven't really studied much yet either. Ehhh. Hopefully it'll look better tomorrow.
Pharmacology Review
• Four Drug Names:
• Generic Name: Name given to drug by first manufacturer prior to approval by government
• Official Name: Name listed in the United States Pharmacopeia
• Chemical Name: Description of drug's exact molecular composition
• Brand Name: Name given to drug by a specific manufacturer
• Four Main Sources of Drugs:
• Animal
• Minerals
• Plants
• Synthetic
• PDR
o Physician Desk Reference - Has package inserts information contained.
• Drug Schedule:
o Schedule I - high abuse potential; may lead to severe dependence; no accepted medical indications; used for research, analysis, or instruction only.
o Schedule II - High abusew potential; may lead to severe dependence; accepted medical indications.
o Schedule III - Less abuse potential than Schedule I and II; may lead to moderate or low physical dependence or high psychological and/or physical dependence; accepted medical indications.
o Schedule IV - Low abuse potential compared to schedule III; limited psychological and/or physical dependence; accepted medical indications
o Schedule V - Lower abuse potential compared to Schedule IV; may lead to limited physical or psychological dependence; accepted medical indication.
• Drug Legislation:
o The Durham-Humphrey Amendments Authorized government to determine drug safety/effectiveness.
Required prescriptions for dangerous drugs.
o Harrison Narcotic Act Controlled import, manufacture, sale of opium, cocaine, derivatives. Required
physicians, pharmacists, manufactures to register with government.
o Pure Food and Drug Act Required accurate labeling of products. Established US Pharmacopeia as the official Information source.
o Controlled Substances Act Authorizes “scheduling” of drugs based on use and abuse potential.
• Test Determines Amount of Given Chemical in Pharmacuticle
o Assay - test that determines the amount and purity of a given chemical in a preparation in the laboratory.
o Bioassy - Test to ascertain a drug’s availability in a biological model.
• 6 Rights to medication Administration
o Right medication
o Right Dose
o Right Time
o Right Route
o Right Patient
o Right Documentation
• Pharmokonetic Processes (LADME, Liberation, absorption ,distribution ,metabolism ,excretion)
o Liberation - the first of five phases of pharmacokinetics.
o Absorption - Absorption is the process by which a medication crosses into the vasculature.
o Distribution - The process of moving the drug from its site of absorption to its site of action.
o (metabolism) Biotransformation - Special name given to the metabolism of drugs.
o Elimination -The process by which drugs are removed from the body.
• Free drug availability - proportion of a drug available in the body to cause either desired or undesired effect.
• Active Transport - requires the use of energy to move a substance.
• Passive Transport - movement of a substance without the use of energy.
• Diffusion - movement a solute into a solution into an area of higher concentration to an area lower concentration.
• Osmosis - movement of a solvent in a solution from an area of lower solute concentration to an area of higher solute concentration.
• Filtration - movement of molecules across a membrane from an area of higher pressure to an area of lower pressure.
• Terotigenic Drug
o Medication that may deform or kill the fetus.
• Mechanisms of Action - Drugs act in four different ways:
o Drugs that act by binding to a receptor site - most drugs oiperate by binding to a receptor.
o Drugs that act by changing physical properties - Drugs change the osmotic balance across membranes are good examples of this type of drug action.
o Drugs that act by chemically combining with other substances - Drugs that participate in che3mical reactions that change the chemical nature of their substrates play a large role in paramedic practice.
o Drugs that act by altering a normal metabolic pathway - Some antcancer and antiviral drugs are chemical analogs of normal metabolic substrates.
• Hepatic First Pass
o The liver’s partial or complete inactivation of a drug before it reaches the systemic circulation.
• Absorption
o Absorption is the process by which a medication crosses into the vasculature. With IV drugs, of course, this process is pretty straightforward. With other routes of administration, however, the medication must somehow cross one or more anatomical barriers to gain access to the circulation. For example, oral medications must cross through the cells of the gastric lining prior to entering the circulation.
The rate of absorption varies tremendously with the specific drug and the conditions of the local environment. Key factors include the pH, the surface area of the absorbing surface and the rate of blood flow to the area.
PH effects are largely those previously described. As a reminder, an acidic drug will best be absorbed in an acidic environment while an alkaline one will best be absorbed in a basic one. A corollary to this is that to decrease the absorption of an acidic drug, increase the pH (‘alkalinize’) the environment and to decrease the absorption of a basic drug, decrease the pH of the environment.
The surface area of the drug affects the rate at which it is absorbed by increasing or decreasing the amount of the drug exposed to the environment for action. If aspirin is taken in tablet form, the surface area is much smaller than if the same amount of drug is taken in powder form. Because the surface area is smaller, much of the drug in the tablet is hidden from the environment by the outer layers. This delays the absorption of the full amount of the drug. On the other hand, this may be a desired effect. Some drugs are given in tablet form with special coatings on them specifically to produce a prolonged release of the drug (technically, this is described as part of the liberation phase).
The surface area of the absorbing environment also is important to determining the rate of absorption. The stomach, while a fairly large organ, has a relatively smooth surface compared to the small intestines giving it a smaller surface area in which little absorption is carried out. The small intestines, on the other hand, have a very large surface area, compounded by the enormous number of villi that further increase surface area. As a result, the vast majority of absorption occurs in the small intestines.
The rate of blood flow also affects the rate of drug absorption. The faster the flow, the faster the absorption. This is largely a result of maintaining a high concentration of drug available for diffusion.
• Blood Brain Barrier
o Tight junctions of the capillary endothelial cells in the central nervous system vasculature. only non-protein-bound, highly lipid-soluble drugs can pass.
• Levodopia
o Absorbed by the dopamine-releasing neuron terminals, where the enzymes decarboxylase metabolizes it into dopamine, thus increasing the amount of dopamine available for release.
• Drug Forms:
o Pills Drugs shaped spherically to be easy to swallow.
o Powders Although they are not as popular as they once were, some powdered drugs are still in use.
o Capsules Gelatin containers enclosing a dose of a drug.
o Suspensions Finely divided drug incorporated in a liquid. Separates on standing.
o Tinctures 10% solution of a drug in alcohol
o Spirits Volatile substance dissolved in alcohol
o Suppositories Drug mixed in a firm base that melts at body temperature
o Solutions One liquid suspended in another. Usually oil in water.
o Elixirs A drug dissolved in water with sugar, flavorings, and alcohol added.
o Tablets Powdered drugs molded or compressed into disks
• Affinity
o Force of attraction between a drug and a receptor.
• Effaciency
o A drug’s ability to cause the expected response
• Agonist
o Drug that binds to a receptor and causes it to initiate the expected response.
• Antagonist
o Drug that binds to a receptor but does not cause it to initiate the expected response.
• Agonist-antagonist
o Drug that binds to a receptor and stimulates some of its effects but blocks others.
o Nubane & Stadal
• Tolerance
o Decreased response to the same amount of drug after repeated administration.
• Latency
o It is the time it takes a drug to have its intended effect, which may depend on the body changing the drug into something effective or just the time it takes for the body to have an effective amount of the drug. Some drugs take hours, others days or weeks to start working.
• Age Affects Absorption of Drug
o The liver and kidney functions of infants are not yet fully developed, so the response to drugs may be altered. Likewise, as we age, the functions of these organs begin to deteriorate. As a result, infants and the elderly are most susceptible to having an altered response to a drug.
• Prototype
o A drug that best demonstrates the class’s common properties and illustrates its particular characteristics.
• Two components of CNS are the Brain and Spinal Cord.
• Placebo Effect - Either consciously or unconsciously, someone (wither the subject or the investigator) reports an effect because they believe there should be one. Study subjects who receive placebos often report feeling better, even though they did not receive any medication.
• Prototype of Opoids
o Agonists is Morphine.
o Antagonist is Narcan.
• Potentiation/Synergism - to enhance or increase the effect of a drug.
• Benzodiazepines are sedative hypnotics.
• Methylxanthines (CNS Stumilants)
o Prototype is Theophylline
o Aminophylline
o Includes Caffine.
• EPS (Extrapyramidal Sympotoms)
o This is a common side effect antipsychotic medications, which include muscle tremor and parkinsonism-like effects.
o Treatment is by use of Benadryl.
• Phenothiazines
o Effectively block dopamine receptors in the CTZ (Chemorecemptor Trigger Zone).
o prochlorperazine (Compazine) and promethazine (Phenergan)
• Butyrophenones
o a chemical compound (a ketone); some of its derivatives are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics.
o Effectively block dopamine receptors in the CTZ (Chemorecemptor Trigger Zone).
o haloperidol (Haldol)
• Acute Dysphonic Reactions
o Dystonic reactions are adverse extrapyramidal effects that often occur shortly after the initiation of neuroleptic drug therapy. These reactions may occur with a wide variety of medications. Dystonic reactions (ie, dyskinesias) are characterized by intermittent spasmodic or sustained involuntary contractions of muscles in the face, neck, trunk, pelvis, and extremities. Dystonic reactions are rarely life threatening, yet are very uncomfortable and often produce significant anxiety and distress for patients.
• SSRIs
o Selective Serotonin Reuptake Inhibitors These drugs’ antidepressants effects are comparable to the TCA’s, but because SSRIs selectively block the reuptake of serotonin, the do not affectdopamine or norepinephrine. Nor do they block histaminic or cholinergic receptors, ths avoiding many of the TCSa’ side effects. The primary adverse reactions to SSRIs are sexual dysfunction, headache, and nauses.
o Prozac, Paxil, Paroxetine (Paxil), Sertralione (Zoloft)
• MAOI
o - (Monoamine Oxidase Inhibitors) metabolizes monoamines into inactive metabolites. MAOIs inhibit monoamine oxidase and block the monoamines’ breakdown, thuys increasing their availability. Monoamine oxidase is also present int eh liver and has a significant role in metabolizing foods that contain tyramine, a substance that increases the release of norepinephrine. The MAOIs’ major side effects is hypertensive crisis brought on by the consumption of foods rich
o Phenelzine (Nardil) is the prototype for this class drug
• Nervous System
o Sympathetic Nervous System
Blood flow to the abdominal organs - Reduction
Peristalsis in the GI tract - Decreased Digestive Activity.
Muscle tone in the urinary bladder wall - Relaction of smooth muscle in the bladder wall.
Glycogen stores in the liver - Release of glucose stores from the liver.
o Parasympathetic Nervous System
Heart rate - Reduction in heart rate and cardiac contractile force.
GI tract gland secretions - Secretion by digestive glands.
Pupils - Constriction.
Muscle tone in the lower airway - Bronchoconstriction.
• Two Main Types of Cholinergic Receptors
o Nictotinic found in all autonomic ganglia.
o Muscurinic found in many organs throughout the body.
• SLUDGE (acronym for Cholinergic Toxicity)
o Salivation
o Lacrimation
o Urination
o Defecation
o gastric motility
o Emesis
• Drugs that paralyze with no sedation?
o Neuromuscular Blockers
They create a state of paralysis without affecting consciousness.
The patient will still know everything that is happening, but won’t be able to move.
• Dopemergic Receptors
o It has been long thought that dopaminergic receptors cause some degree of dilation of the renal, coronary, and cerebral arteries. However, recent studies have questioned whether such an effect exists. Several studies have demonstrated that low-dose dopamine infusions actually worsen renal function instead of improving it. Other studies have not been able to demonstrate improvide bowel perfusion with dopamine administration.
• Terbutaline:
o Used to treat asthma.
o Helps with Bronchodilitation, relaxes bronchial smooth muscle by action on B2 receptors with less effect on heart rate
o It’s a Beta2 adrenergic agonist
• Lidocaine
o A sodium Channel Blocker
o Slows conduction through ventricles, Increases rate of repolarization, reduces automaticity. Class 1b
• Procainamide
o Antiarrhythmic agent class 1a.
o Widens QRS and QT interval.
o Side effects are asystole
• What system in the body controls fluid?
• Antihyperlipidemics
o drugs used to lower cholesterol levels in the body
• Thrombolytic Agents
o act directly on thrombi to break them up. End in ASE normally
• Beta2
o Albuteral (Proventil)
• Antitusses
o Medication that suppresses the stimulus to cough in the CNS.
o Expectorant produces productivity and Mucolytics water down the mucus.
• Oxytocin
o a mammalian hormone that also acts as a neurotransmitter in the brain. It is best known for its roles in female reproduction: it is released in large amounts after distension of the cervix and vagina during labor, and after stimulation of the nipples, facilitating birth and breastfeeding, respectively. Recent studies have begun to investigate oxytocin's role in various behaviors, including orgasm, social recognition, pair bonding, anxiety, trust, love, and maternal behaviors.
• Pancreatic Hormone
o Glucagon- made in pancreas in alpha cells. Increases blood glucose level. Increases glycogen breakdown into glucose.
o Insulin - is a hormone that has extensive effects on metabolism and other body functions, such as vascular compliance. Insulin causes cells in the liver, muscle, and fat tissue to take up glucose from the blood, storing it as glycogen in the liver and muscle, and stopping use of fat as an energy source. When insulin is absent (or low), glucose is not taken up by body cells, and the body begins to use fat as an energy source, for example, by transfer of lipids from adipose tissue to the liver for mobilization as an energy source. As its level is a central metabolic control mechanism, its status is also used as a control signal to other body systems (such as amino acid uptake by body cells). It has several other anabolic effects throughout the body. When control of insulin levels fails, diabetes mellitus will result.
• Vaccine
o A solution containing a modified pathogen that does not actually cause disease but still stimulates the development of antibodies specific to it.
• Atropine
o Hot as hell, blind as a bat, mad as a hatter, red as a beet
o Used as an antidote for Cholinergic Toxicity
o toxic overdosage (see Adverse Effects), a short-acting barbiturate or diazepam may be given as needed to control marked excitement and convulsions. Large doses for sedation should be avoided because central depressant action may coincide with the depression occurring late in atropine poisoning. Central stimulants are not recommended.
• GABA - gamma aminobutyric acid.
o Chief inhibitory neurotransmitter in the CNS. GABA receptors are dispersed on proteins that make up chlorideion channels in the cell membrane. Allows for chloride to enter the cell and hyperpolarizes the membrane. By hyper polarizing the membrane depolarization in more difficult. Benzos, Barbs increase GABBA receptor chloride ion channel complexes’ potential for binding with GABA.
• Phases of Fast Action Potential
o Fast potentials are found in the Myocardial Contractile Tissues
o Phase 0 - represents Depolarization, results from a rapid influx of Na+ ions into the cell.
o Phase 1 - K+ begins to leave the cell, slowly returning the cell to its normal negative charge.
o Phase 2 - Interrupts with an influx of Ca++ into the cell.
o Phase 3 - is marked by a cessation of calcium influx and the rapid efflux of potassium.
o Phase 4 - is normally a flat stage representing the resting membrane potential. However, in pathologic states is may include a slow influx of sodium that will gradually make the inside of the cell more positive.
• Phases of Slow Action Potential
o Slow action potentials are found in the AV and SA nodes
o The slow potentials are similar to the fast ones, have several important distinctions.
They are located in the dominant pacemakers of the heart (AV and SA nodes).
They depolarize differently.
o Phase 4 exhibits a gradual increasing slope towards threshold potential. A gradual influx of calcium into the cell causes depolarization.
• Calcium Channel Blockers
o ↓ Calcium influx causes a ↓ in automaticity.
o Most usefulness is from decreasing conductivity through the AV node in patients with preserved ventricular function. They effectively slow the ventricular conduction of atrial fibrillation and flutter, and they terminate Super Ventricular Tachycardias originating from a reentrant circuit. Verapamil (Calan) and Diltiazem (Cardizem) are the only two calcium channel blockers that affect the heart Verapamil is a prototype. Nephedapine has no heart effects.
• Blood Pressure is affected by the RAAS (Renin-Angiotensin-Aldosterone System).
• Drugs to Know -
o diltiazem (Cardizim) - Calcium Channel Blocker - Directly affects heart.
o carbamazepine (Tegritol)- anticonvulsant, limits Na ion across membrane related to TCAs
o diazepam (Valuim)- benzodiazepine, binds to stereospecific benzo receptors on GABA
o alprazelam(Xanax)-benzodiazepine, binds to stereospecific benzo receptors on GABA
o lorazepam(Ativan)- benzodiazepine, binds to stereospecific benzo receptors on GABA,
o midazelam(Versed)- benzodiazepine, binds to stereospecific benzo receptors on GABA
o furosemide(Lasix)- loop diaretic, inhibits reabsorbtion of Na and Cl on the ascending loop of henle
o amnitriptyline(Elavil)-TCA, increases synaptic concentration of serotonin and norepi in CNSby inhibiting the reuptake.
o warfrin(Coumadine)-anticoagulant, vitamin K antagonist,
o digoxin(Lenoxin)-antiarrythmic agent class IV, cardiac glycoside
o lisinopril(Zestril)-ACE inhibitor
o carvedilol(Coreg)- Beta blocker w/ alpha blocking activity
o naloxone(Narcan)- opiod antagonist
o olanzapine(zyprexa)-antipsychotic agent,
o ketoralac(Toradol)-NSAID
o EXTRAS PROVIDED:
pioglitazone(Actos)-antidiabetic agent
adrenalin(epinephrine)- alpha beta agonist
ramipril(Altase)-ACE inhibitor
succinylcholine- depolarizing neuromuscular blocker agent
donepizil(Aricept)-Acetylcholinesterase inhibitor
diphenhydromine(Benadryl)-Histamine 1 antagonist
captopril(Capoten)-ACE inhibitor
diltiazem(Cardizem)-Ca+ channel blocker Class IV
metformin(Glucophage)- antidiabetic agent
verapamil(Isoptin)- antiarrhythmic agent class IV Ca+ channel blocker
lamotrigine(Lamictal)- anticonvulant
norepinephrine(Levophed)- Alpha beta agonist
atorvasatin(Lipitor)-Antilipemic
vecuronium(Norcuron)- Nondepolarizing neuromuscular blocker agent
pantoprazole(Protonix)- Proton pump inhibitor
Resperidone(Riperdal)- anti manic/psychotic agent
Propafenone(Rythmol)- antiarrythemic Class Ic
Quetiapine(Seroquel)-antipsychotic agent
Carbamazepine(Tegretol)- anticonvulsant
Lidocaine(Xylocaine)-topical analgesic, Na channel blocker class Ib
Olanzapine(zyprexa)-anti manic/psychotic agent
Phenelzine(Nardil)- MAOI
The reviewing I've been doing just got a whole lot less scary, which makes me wish I'd started earlier :P You'll be happy for the cut :P
The latest gossip in the class is about some of the other young'ins. A, who recently turned into the jack ass of the class(thank goodness really, for the longest time I thought I was the only one that hated him....), and W, who is the pretty one, really, which is the only thing about her that really sticks out. She doesn't say anything of sustanence or quality, and never smiles at anyone but A. M told me that W has been spending every waking moment that she's not sleeping or working at A's office, at a private medical response company. It bothers the other employees, including M and L, who work there. The bad part is, that W will go on calls with them and everything, and start IVs and whatnot, which neither of them is ceritified to do right now, so it's very illegal and dangerous, on top of the fact that A is married, and for less than 4 months at that. A told me that they get out their books and pretend to study when anyone else walks in. No one knows if there's something between them or not, but it's fishy.
Most of the ER nurses don't even like A, lol. A's buddy D is ok, but he can be an ass too.
So that's that part. I haven't been sleeping well, but hopefully I'll go to bed soon and start on this again tomorrow. Hopefully the retest won't be too soon either. :P
I want my break to start, but I haven't really studied much yet either. Ehhh. Hopefully it'll look better tomorrow.
Pharmacology Review
• Four Drug Names:
• Generic Name: Name given to drug by first manufacturer prior to approval by government
• Official Name: Name listed in the United States Pharmacopeia
• Chemical Name: Description of drug's exact molecular composition
• Brand Name: Name given to drug by a specific manufacturer
• Four Main Sources of Drugs:
• Animal
• Minerals
• Plants
• Synthetic
• PDR
o Physician Desk Reference - Has package inserts information contained.
• Drug Schedule:
o Schedule I - high abuse potential; may lead to severe dependence; no accepted medical indications; used for research, analysis, or instruction only.
o Schedule II - High abusew potential; may lead to severe dependence; accepted medical indications.
o Schedule III - Less abuse potential than Schedule I and II; may lead to moderate or low physical dependence or high psychological and/or physical dependence; accepted medical indications.
o Schedule IV - Low abuse potential compared to schedule III; limited psychological and/or physical dependence; accepted medical indications
o Schedule V - Lower abuse potential compared to Schedule IV; may lead to limited physical or psychological dependence; accepted medical indication.
• Drug Legislation:
o The Durham-Humphrey Amendments Authorized government to determine drug safety/effectiveness.
Required prescriptions for dangerous drugs.
o Harrison Narcotic Act Controlled import, manufacture, sale of opium, cocaine, derivatives. Required
physicians, pharmacists, manufactures to register with government.
o Pure Food and Drug Act Required accurate labeling of products. Established US Pharmacopeia as the official Information source.
o Controlled Substances Act Authorizes “scheduling” of drugs based on use and abuse potential.
• Test Determines Amount of Given Chemical in Pharmacuticle
o Assay - test that determines the amount and purity of a given chemical in a preparation in the laboratory.
o Bioassy - Test to ascertain a drug’s availability in a biological model.
• 6 Rights to medication Administration
o Right medication
o Right Dose
o Right Time
o Right Route
o Right Patient
o Right Documentation
• Pharmokonetic Processes (LADME, Liberation, absorption ,distribution ,metabolism ,excretion)
o Liberation - the first of five phases of pharmacokinetics.
o Absorption - Absorption is the process by which a medication crosses into the vasculature.
o Distribution - The process of moving the drug from its site of absorption to its site of action.
o (metabolism) Biotransformation - Special name given to the metabolism of drugs.
o Elimination -The process by which drugs are removed from the body.
• Free drug availability - proportion of a drug available in the body to cause either desired or undesired effect.
• Active Transport - requires the use of energy to move a substance.
• Passive Transport - movement of a substance without the use of energy.
• Diffusion - movement a solute into a solution into an area of higher concentration to an area lower concentration.
• Osmosis - movement of a solvent in a solution from an area of lower solute concentration to an area of higher solute concentration.
• Filtration - movement of molecules across a membrane from an area of higher pressure to an area of lower pressure.
• Terotigenic Drug
o Medication that may deform or kill the fetus.
• Mechanisms of Action - Drugs act in four different ways:
o Drugs that act by binding to a receptor site - most drugs oiperate by binding to a receptor.
o Drugs that act by changing physical properties - Drugs change the osmotic balance across membranes are good examples of this type of drug action.
o Drugs that act by chemically combining with other substances - Drugs that participate in che3mical reactions that change the chemical nature of their substrates play a large role in paramedic practice.
o Drugs that act by altering a normal metabolic pathway - Some antcancer and antiviral drugs are chemical analogs of normal metabolic substrates.
• Hepatic First Pass
o The liver’s partial or complete inactivation of a drug before it reaches the systemic circulation.
• Absorption
o Absorption is the process by which a medication crosses into the vasculature. With IV drugs, of course, this process is pretty straightforward. With other routes of administration, however, the medication must somehow cross one or more anatomical barriers to gain access to the circulation. For example, oral medications must cross through the cells of the gastric lining prior to entering the circulation.
The rate of absorption varies tremendously with the specific drug and the conditions of the local environment. Key factors include the pH, the surface area of the absorbing surface and the rate of blood flow to the area.
PH effects are largely those previously described. As a reminder, an acidic drug will best be absorbed in an acidic environment while an alkaline one will best be absorbed in a basic one. A corollary to this is that to decrease the absorption of an acidic drug, increase the pH (‘alkalinize’) the environment and to decrease the absorption of a basic drug, decrease the pH of the environment.
The surface area of the drug affects the rate at which it is absorbed by increasing or decreasing the amount of the drug exposed to the environment for action. If aspirin is taken in tablet form, the surface area is much smaller than if the same amount of drug is taken in powder form. Because the surface area is smaller, much of the drug in the tablet is hidden from the environment by the outer layers. This delays the absorption of the full amount of the drug. On the other hand, this may be a desired effect. Some drugs are given in tablet form with special coatings on them specifically to produce a prolonged release of the drug (technically, this is described as part of the liberation phase).
The surface area of the absorbing environment also is important to determining the rate of absorption. The stomach, while a fairly large organ, has a relatively smooth surface compared to the small intestines giving it a smaller surface area in which little absorption is carried out. The small intestines, on the other hand, have a very large surface area, compounded by the enormous number of villi that further increase surface area. As a result, the vast majority of absorption occurs in the small intestines.
The rate of blood flow also affects the rate of drug absorption. The faster the flow, the faster the absorption. This is largely a result of maintaining a high concentration of drug available for diffusion.
• Blood Brain Barrier
o Tight junctions of the capillary endothelial cells in the central nervous system vasculature. only non-protein-bound, highly lipid-soluble drugs can pass.
• Levodopia
o Absorbed by the dopamine-releasing neuron terminals, where the enzymes decarboxylase metabolizes it into dopamine, thus increasing the amount of dopamine available for release.
• Drug Forms:
o Pills Drugs shaped spherically to be easy to swallow.
o Powders Although they are not as popular as they once were, some powdered drugs are still in use.
o Capsules Gelatin containers enclosing a dose of a drug.
o Suspensions Finely divided drug incorporated in a liquid. Separates on standing.
o Tinctures 10% solution of a drug in alcohol
o Spirits Volatile substance dissolved in alcohol
o Suppositories Drug mixed in a firm base that melts at body temperature
o Solutions One liquid suspended in another. Usually oil in water.
o Elixirs A drug dissolved in water with sugar, flavorings, and alcohol added.
o Tablets Powdered drugs molded or compressed into disks
• Affinity
o Force of attraction between a drug and a receptor.
• Effaciency
o A drug’s ability to cause the expected response
• Agonist
o Drug that binds to a receptor and causes it to initiate the expected response.
• Antagonist
o Drug that binds to a receptor but does not cause it to initiate the expected response.
• Agonist-antagonist
o Drug that binds to a receptor and stimulates some of its effects but blocks others.
o Nubane & Stadal
• Tolerance
o Decreased response to the same amount of drug after repeated administration.
• Latency
o It is the time it takes a drug to have its intended effect, which may depend on the body changing the drug into something effective or just the time it takes for the body to have an effective amount of the drug. Some drugs take hours, others days or weeks to start working.
• Age Affects Absorption of Drug
o The liver and kidney functions of infants are not yet fully developed, so the response to drugs may be altered. Likewise, as we age, the functions of these organs begin to deteriorate. As a result, infants and the elderly are most susceptible to having an altered response to a drug.
• Prototype
o A drug that best demonstrates the class’s common properties and illustrates its particular characteristics.
• Two components of CNS are the Brain and Spinal Cord.
• Placebo Effect - Either consciously or unconsciously, someone (wither the subject or the investigator) reports an effect because they believe there should be one. Study subjects who receive placebos often report feeling better, even though they did not receive any medication.
• Prototype of Opoids
o Agonists is Morphine.
o Antagonist is Narcan.
• Potentiation/Synergism - to enhance or increase the effect of a drug.
• Benzodiazepines are sedative hypnotics.
• Methylxanthines (CNS Stumilants)
o Prototype is Theophylline
o Aminophylline
o Includes Caffine.
• EPS (Extrapyramidal Sympotoms)
o This is a common side effect antipsychotic medications, which include muscle tremor and parkinsonism-like effects.
o Treatment is by use of Benadryl.
• Phenothiazines
o Effectively block dopamine receptors in the CTZ (Chemorecemptor Trigger Zone).
o prochlorperazine (Compazine) and promethazine (Phenergan)
• Butyrophenones
o a chemical compound (a ketone); some of its derivatives are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics.
o Effectively block dopamine receptors in the CTZ (Chemorecemptor Trigger Zone).
o haloperidol (Haldol)
• Acute Dysphonic Reactions
o Dystonic reactions are adverse extrapyramidal effects that often occur shortly after the initiation of neuroleptic drug therapy. These reactions may occur with a wide variety of medications. Dystonic reactions (ie, dyskinesias) are characterized by intermittent spasmodic or sustained involuntary contractions of muscles in the face, neck, trunk, pelvis, and extremities. Dystonic reactions are rarely life threatening, yet are very uncomfortable and often produce significant anxiety and distress for patients.
• SSRIs
o Selective Serotonin Reuptake Inhibitors These drugs’ antidepressants effects are comparable to the TCA’s, but because SSRIs selectively block the reuptake of serotonin, the do not affectdopamine or norepinephrine. Nor do they block histaminic or cholinergic receptors, ths avoiding many of the TCSa’ side effects. The primary adverse reactions to SSRIs are sexual dysfunction, headache, and nauses.
o Prozac, Paxil, Paroxetine (Paxil), Sertralione (Zoloft)
• MAOI
o - (Monoamine Oxidase Inhibitors) metabolizes monoamines into inactive metabolites. MAOIs inhibit monoamine oxidase and block the monoamines’ breakdown, thuys increasing their availability. Monoamine oxidase is also present int eh liver and has a significant role in metabolizing foods that contain tyramine, a substance that increases the release of norepinephrine. The MAOIs’ major side effects is hypertensive crisis brought on by the consumption of foods rich
o Phenelzine (Nardil) is the prototype for this class drug
• Nervous System
o Sympathetic Nervous System
Blood flow to the abdominal organs - Reduction
Peristalsis in the GI tract - Decreased Digestive Activity.
Muscle tone in the urinary bladder wall - Relaction of smooth muscle in the bladder wall.
Glycogen stores in the liver - Release of glucose stores from the liver.
o Parasympathetic Nervous System
Heart rate - Reduction in heart rate and cardiac contractile force.
GI tract gland secretions - Secretion by digestive glands.
Pupils - Constriction.
Muscle tone in the lower airway - Bronchoconstriction.
• Two Main Types of Cholinergic Receptors
o Nictotinic found in all autonomic ganglia.
o Muscurinic found in many organs throughout the body.
• SLUDGE (acronym for Cholinergic Toxicity)
o Salivation
o Lacrimation
o Urination
o Defecation
o gastric motility
o Emesis
• Drugs that paralyze with no sedation?
o Neuromuscular Blockers
They create a state of paralysis without affecting consciousness.
The patient will still know everything that is happening, but won’t be able to move.
• Dopemergic Receptors
o It has been long thought that dopaminergic receptors cause some degree of dilation of the renal, coronary, and cerebral arteries. However, recent studies have questioned whether such an effect exists. Several studies have demonstrated that low-dose dopamine infusions actually worsen renal function instead of improving it. Other studies have not been able to demonstrate improvide bowel perfusion with dopamine administration.
• Terbutaline:
o Used to treat asthma.
o Helps with Bronchodilitation, relaxes bronchial smooth muscle by action on B2 receptors with less effect on heart rate
o It’s a Beta2 adrenergic agonist
• Lidocaine
o A sodium Channel Blocker
o Slows conduction through ventricles, Increases rate of repolarization, reduces automaticity. Class 1b
• Procainamide
o Antiarrhythmic agent class 1a.
o Widens QRS and QT interval.
o Side effects are asystole
• What system in the body controls fluid?
• Antihyperlipidemics
o drugs used to lower cholesterol levels in the body
• Thrombolytic Agents
o act directly on thrombi to break them up. End in ASE normally
• Beta2
o Albuteral (Proventil)
• Antitusses
o Medication that suppresses the stimulus to cough in the CNS.
o Expectorant produces productivity and Mucolytics water down the mucus.
• Oxytocin
o a mammalian hormone that also acts as a neurotransmitter in the brain. It is best known for its roles in female reproduction: it is released in large amounts after distension of the cervix and vagina during labor, and after stimulation of the nipples, facilitating birth and breastfeeding, respectively. Recent studies have begun to investigate oxytocin's role in various behaviors, including orgasm, social recognition, pair bonding, anxiety, trust, love, and maternal behaviors.
• Pancreatic Hormone
o Glucagon- made in pancreas in alpha cells. Increases blood glucose level. Increases glycogen breakdown into glucose.
o Insulin - is a hormone that has extensive effects on metabolism and other body functions, such as vascular compliance. Insulin causes cells in the liver, muscle, and fat tissue to take up glucose from the blood, storing it as glycogen in the liver and muscle, and stopping use of fat as an energy source. When insulin is absent (or low), glucose is not taken up by body cells, and the body begins to use fat as an energy source, for example, by transfer of lipids from adipose tissue to the liver for mobilization as an energy source. As its level is a central metabolic control mechanism, its status is also used as a control signal to other body systems (such as amino acid uptake by body cells). It has several other anabolic effects throughout the body. When control of insulin levels fails, diabetes mellitus will result.
• Vaccine
o A solution containing a modified pathogen that does not actually cause disease but still stimulates the development of antibodies specific to it.
• Atropine
o Hot as hell, blind as a bat, mad as a hatter, red as a beet
o Used as an antidote for Cholinergic Toxicity
o toxic overdosage (see Adverse Effects), a short-acting barbiturate or diazepam may be given as needed to control marked excitement and convulsions. Large doses for sedation should be avoided because central depressant action may coincide with the depression occurring late in atropine poisoning. Central stimulants are not recommended.
• GABA - gamma aminobutyric acid.
o Chief inhibitory neurotransmitter in the CNS. GABA receptors are dispersed on proteins that make up chlorideion channels in the cell membrane. Allows for chloride to enter the cell and hyperpolarizes the membrane. By hyper polarizing the membrane depolarization in more difficult. Benzos, Barbs increase GABBA receptor chloride ion channel complexes’ potential for binding with GABA.
• Phases of Fast Action Potential
o Fast potentials are found in the Myocardial Contractile Tissues
o Phase 0 - represents Depolarization, results from a rapid influx of Na+ ions into the cell.
o Phase 1 - K+ begins to leave the cell, slowly returning the cell to its normal negative charge.
o Phase 2 - Interrupts with an influx of Ca++ into the cell.
o Phase 3 - is marked by a cessation of calcium influx and the rapid efflux of potassium.
o Phase 4 - is normally a flat stage representing the resting membrane potential. However, in pathologic states is may include a slow influx of sodium that will gradually make the inside of the cell more positive.
• Phases of Slow Action Potential
o Slow action potentials are found in the AV and SA nodes
o The slow potentials are similar to the fast ones, have several important distinctions.
They are located in the dominant pacemakers of the heart (AV and SA nodes).
They depolarize differently.
o Phase 4 exhibits a gradual increasing slope towards threshold potential. A gradual influx of calcium into the cell causes depolarization.
• Calcium Channel Blockers
o ↓ Calcium influx causes a ↓ in automaticity.
o Most usefulness is from decreasing conductivity through the AV node in patients with preserved ventricular function. They effectively slow the ventricular conduction of atrial fibrillation and flutter, and they terminate Super Ventricular Tachycardias originating from a reentrant circuit. Verapamil (Calan) and Diltiazem (Cardizem) are the only two calcium channel blockers that affect the heart Verapamil is a prototype. Nephedapine has no heart effects.
• Blood Pressure is affected by the RAAS (Renin-Angiotensin-Aldosterone System).
• Drugs to Know -
o diltiazem (Cardizim) - Calcium Channel Blocker - Directly affects heart.
o carbamazepine (Tegritol)- anticonvulsant, limits Na ion across membrane related to TCAs
o diazepam (Valuim)- benzodiazepine, binds to stereospecific benzo receptors on GABA
o alprazelam(Xanax)-benzodiazepine, binds to stereospecific benzo receptors on GABA
o lorazepam(Ativan)- benzodiazepine, binds to stereospecific benzo receptors on GABA,
o midazelam(Versed)- benzodiazepine, binds to stereospecific benzo receptors on GABA
o furosemide(Lasix)- loop diaretic, inhibits reabsorbtion of Na and Cl on the ascending loop of henle
o amnitriptyline(Elavil)-TCA, increases synaptic concentration of serotonin and norepi in CNSby inhibiting the reuptake.
o warfrin(Coumadine)-anticoagulant, vitamin K antagonist,
o digoxin(Lenoxin)-antiarrythmic agent class IV, cardiac glycoside
o lisinopril(Zestril)-ACE inhibitor
o carvedilol(Coreg)- Beta blocker w/ alpha blocking activity
o naloxone(Narcan)- opiod antagonist
o olanzapine(zyprexa)-antipsychotic agent,
o ketoralac(Toradol)-NSAID
o EXTRAS PROVIDED:
pioglitazone(Actos)-antidiabetic agent
adrenalin(epinephrine)- alpha beta agonist
ramipril(Altase)-ACE inhibitor
succinylcholine- depolarizing neuromuscular blocker agent
donepizil(Aricept)-Acetylcholinesterase inhibitor
diphenhydromine(Benadryl)-Histamine 1 antagonist
captopril(Capoten)-ACE inhibitor
diltiazem(Cardizem)-Ca+ channel blocker Class IV
metformin(Glucophage)- antidiabetic agent
verapamil(Isoptin)- antiarrhythmic agent class IV Ca+ channel blocker
lamotrigine(Lamictal)- anticonvulant
norepinephrine(Levophed)- Alpha beta agonist
atorvasatin(Lipitor)-Antilipemic
vecuronium(Norcuron)- Nondepolarizing neuromuscular blocker agent
pantoprazole(Protonix)- Proton pump inhibitor
Resperidone(Riperdal)- anti manic/psychotic agent
Propafenone(Rythmol)- antiarrythemic Class Ic
Quetiapine(Seroquel)-antipsychotic agent
Carbamazepine(Tegretol)- anticonvulsant
Lidocaine(Xylocaine)-topical analgesic, Na channel blocker class Ib
Olanzapine(zyprexa)-anti manic/psychotic agent
Phenelzine(Nardil)- MAOI