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The area of pharmocology that refers to the use of specific drugs to prevent, treat, or diagnose a disease. |
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The study of how the body deals with the drug in terms of the way it is absorbed, distributed, and eliminated. |
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The study of harmful effects of chemicals. |
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The official or nonproprietary name. Tends to be somewhat shorter and is often derived from the chemical name. |
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The brand name that is assigned to the compound by the pharmaceutical company and may or may not bear any reference at all to the chemical and generic terminology. |
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If there is no existing patent for that compound or if the patent has expired, can the same drug be marketed by separate drug companies? |
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1. Should undergo testing to establish that it has the same type and amount of active ingredients 2. The same administration route 3. Same pharmacokinetic profile 4. Same therapeutic effects as brand name. |
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Which phase of clinical studies is this? The drug is usually tested with a small number of healthy volunteers. |
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Which phase of clinical studies is this? The drug is tested in a relatively small sample (200-300) with a specific disease or pathological condition. |
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Which phase of clinical studies is this? Clinical evaluation is expanded to include more patients (several hundred to several thousand) as well as more evaluators. |
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Meds used to treat relatively minor problems and make the consumer more comfortable until the condition is resolved. Non-prescription drugs that can be purchased directly by the consumer. |
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The point at which there is no further increase in the response of the drug |
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Ceiling Effect Maximal Efficacy |
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Related to the dose that produces a given response in a specific amplitude. |
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When two drugs ae compared, the __ potent drug requires a lower dose to produce the same effect as the higher dose of the second drug. |
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The dose at which 50% of the population respond to the drug in a specified manner |
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The dose at which 50% of the group exhibits the adverse effect |
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T1 = TD/ED. Uses the median effective and toxic doses. The greater the value of T1, the safer the drug is considered to be. |
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Drugs that are given orally are subject to a phenomenon known as what? This means that the drug is metabolized in the liver prior to reaching its target tissue. |
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Name two common routes of drug administration. |
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What does parenteral mean? |
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Does not use the GI tract |
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Name the Enteral routes of drug administration. |
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Name 4 parenteral routes of drug administration |
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Definition
Inhalation Injection Topical Transdermal |
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Iontophoresis and phonophoresis are administered via which route? |
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The extent to which the drug reaches the systemic circulation is referred to as ___, which is a parameter expressed as the percentage of the drug administered that reaches the bloodstream. |
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Drugs will diffuse more rapidly if they are in their __, __ form |
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The special case of the diffusion where the diffusion substance is water. |
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Name 3 characteristics of active transport. |
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-Carrier specificity -Expenditure of energy -Ability to transport substances against a concentration gradient |
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The primary site for drug storage in the body is __ tissue. |
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The amount of drug administered divided by the concentration of drug in plasma |
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A normal 70kg man has a total body fluid content of ~42L (5.5L blood). If the calculated Vd of a drug is approx equal to the total amount of body water, then the drug is distributed uniformly througout where? |
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Refers to chemical changes that take place in the drug following administration. |
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Definition
Biotransformation/Drug Metabolism |
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Biotransformation usually results in an altered version of the original compound known as __, which is usually inactive or has a greatly reduced level of pharmacologic activity. |
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Occurs when either oxygen is added or hydrogen is removed from the original compound. |
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The original compound is broken into separate parts. |
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Where is the primary location for drug metabolism? |
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Prolonged use of certain drugs "induces" the body to be able to enzymatically destroy the drug more rapidly, usually because either more metabolizing enzymes are being manufactured or less are being degraded. May cause drugs to be metabolized more rapidly than expected, thus decreasing their therapeutic effect. |
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One reason why tolerance to some drugs occurs when it is used for extended periods (tolerance is the need for increased drug dosages to produce the same effect). |
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One reason why tolerance to some drugs occurs when it is used for extended periods (tolerance is the need for increased drug dosages to produce the same effect). |
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The primary site for drug excretion |
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Can be described either in terms of all organ's and tissue's ability to eliminate the drug (systemic) or in terms of a single organ or tissue's ability to eliminate the drug. |
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The amount of time required for 50% of the drug remaining in the body to be eliminated. |
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Name 7 variations in drug response and metabolism |
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Definition
1. Genetic Factors 2. Disease 3. Drug Interactions 4. Age 5. Diet 6. Gender 7. Other Factors |
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The principle site for receptors that recognize endogenous and exogenous compounds is the what? |
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Definition
Outer surface of the cell membrane |
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When bound by ACh molecules, the receptor activates and opens a pore through the cell membrane, thereby increasing the permeability of the muscle cell to Na+ |
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Activated by binding guanine nucleotides. When a substance binds to the surface receptor, the receptor moves laterally in the cell membrane and attaches to a G protein - cyclic AMP acts as the second messenger in this sytem by activating other enzymes. |
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An enzyme that is located on the inner surface of the cell membrane, is responsible for hydrolyzing adenosine triphosphate (ATP) into cAMP. |
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The amount of attraction between a drug and a receptor. A drug with high __ binds readily to open receptors, even if the concentration of the drug is relatively low. |
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A drug that can bind to the receptor and initiate a change in cell function. Has affinity and efficacy. |
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Often calle "blockers" because they block the effect of another chemical, preventing change in cell function. Only has affinity. |
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Both the agonist and antagonist have an equal opportunity to occupy the ___. |
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Form strong, essentially permanent bond to the receptor. Have either extremely high affinity for the receptor or actually form irreversible covalent bonds to the receptor. |
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Noncompetitive Antagonists |
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The noncompetitive antagonist cannot be displaced by the agonist, regardless of how much the agonist is present. Thus the term ___ refers to the inability of the agonist to compete with the antagonist for the recptor site. The obvious disadvantage to this type of receptor blocker is that the inhibition cannot be overcome in cases of an overdose of the antagonist. |
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Drugs are classified as this when they do not evoke a maximal response compared to a strong agonists. Still occupies all available receptors. |
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A fairly brief and transient decrease in responsiveness. Decrease in appropriate receptor population through prolonged stimulation. |
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A slower, more prolonged process in which the actual number of available receptors is diminished. |
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Drugs that are classified as __ are used both to relax the patient and to promote sleep. |
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Exert their effects by increasing the inhibitory effects of GABA in CNS. GABA typically exerts its inhibitory effects by binding to its receptor site and initiating an increase in Cl- conductance. |
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When used in sedative-hypnotic doses, __ may function in a similar fasion to the bensodiazepines in that they also potentiate the inhibitory effects of GABA. |
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Residual (hangover) effects can be resolved somewhat by: (3) |
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Definition
1. Taking a smaller dose 2. Using a drug with a shorter half-life 3. Newer drugs appear to have milder effects, due to short half-life and limited action duration |
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Withdrawal after short-term benzodiazepine use may be associated with problems such as sleep disturbances or so-called __ __ |
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Buspirone does not act on the __ receptor, but exerts its antianxiety effects by increasing the effects of serotonin in certain areas of the brain. |
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Valium increases its inhibitory effects of ___. |
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Certain antidepressants such as Paxil and Effexor can help reduce anxiety independent of their effects on __. The antidepressants ahve therefore been advocated as an alternative treatment for anxiety, especially for people who cannot tolerate the side effects of traditional antiolytics, or who might be especially susceptible to the addictive properties of drugs like the ___ |
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Definition
Depression Bensodiazepines |
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Transmitter for depression |
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Definition
Epinephrine and Norepinephrine |
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These drugs work by blocking the reuptake of amine neurotransmitters into the presynaptic terminal |
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An enzyme that is located at amine synapses and helps removed released transmitters through enzymatic destruction. Drugs that inhibit this enzyme allow more of the transmitter to remain in the synaptic cleft and continue to exert an effect. |
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Second-generation drugs that selectively block the reuptake of serotonin. |
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SSRI's (Selective Serotonin Reuptake Inhibitors) |
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Serotonin syndrome is characterized by what 5 things? |
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Definition
Sweating Shivering Movement Disorders Muscle Fasciculations Other neuromuscular Stuff |
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Traditional __ medications such as amitriptyline and nortriptyline are often considered the drugs of choice for chronic pain |
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The primary form of drug treatment for bipolar disorder consists of what? |
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This is not metabolized, and drug elimination takes place almost exclusively through excretion in the urine. |
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Improvement in mood may occur within __ weeks after beginning antidepressant drug treatment, but these agents must often be administered for 1 __ or more before an appreciable improvement in symptoms occur. |
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** we had some question where this was the answer ** |
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Appears to be caused by an overactivity of dopamine pathways in certain parts of hte brain such as the limbic system. |
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These are used to successfully treat schizophrenia block central dopamine receptors to some extent. It is a dopamine receptor antagonist. |
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Newer __ agents do not block the D2 receptors in the basal ganglia as strongly as conventional antipsychotics, hence their reduced risk of motor side effects. |
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__ are often used in Alzheimer disease and other cases of dementia to help control aggression and agitation. |
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One of the more seriuos problems occurring from the use of antipsychotics is the production of abnormal movement patterns |
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Characterized by the number of involuntary and fragmented movements. It is the most feared side effect of antipsychotic drugs. Drug-induced __ __ appears irreversible. |
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Name 5 Extrapyramidal Symptoms |
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Definition
Tardive Dyskinesia Pseudoparkinsonism Akathisia Dyskinesia and Dystonias Meuroleptic Malignant Syndrome |
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Patients taking relatively high doses of the more potent antipsychotics |
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Neuroleptic Malignant Syndrome |
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Name 3 types of Partial Seizures |
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Definition
1. Simple Partial 2. Complex Partial 3. Partial becoming Generalized |
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Name 6 types of Generalized Seizures |
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Definition
1. Absence (petit mal) 2. Myoclonic 3. Clonic 4. Tonic 5. Tonic-Clonic 6. Atonic |
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Limited (focal) motor or sensory signs (convulsions confined to one limb, specific sensory hallucinations); consciousness remains intact |
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Consciousness impaired; bizarre behavior; wide variety of other manifestations; specific electroenchephalography abnormality |
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Symptoms progressively increase until seizure resembles a generalized (tonic-clonic) seizure |
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Definition
Partial becoming generalized |
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Sudden, brief loss of consciousness; motor signs may be absent or may range from rapid eye-blinking to symmetrical jerking movements of entire body |
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Definition
Absence (petit mal) seizures |
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Sudden, brief, "shock-like" contractions of muscles in the face and trunk, or in one or more extremeties; contractions may be single or multiple; consciousness may be impaired |
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Rhythmic, synchronized contractions throughout hte body; loss of consciousness |
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Generalized sustained muscle contractions throughout body; loss of consciousness |
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Major convulsions of entire body; sustained contraction of all muscles followed by powerful rhythmic contractions; loss of consciousness |
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Definition
Tonic-Clonic (grand mal) seizures |
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Sudden loss of muscle tone in the head and neck, one limb, or throughout the entire body; consciousness may be maintained or lost briefly. |
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Epileptic drugs try to inhibit firing of certain neurons by: (3) |
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Definition
1. Increasing the inhibitory effects of GABA 2. Decreasing the effects of excitatory amino acids 3. Altering the movement of ions across the neuronal membrane |
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What is the primary problem with antiepileptic drugs? |
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Antiepileptics mainly work by inhibiting what? |
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Name 2 bensodiazepines that work as an antiepileptic |
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Definition
Klonopin (Clonazepam) Tranxene (Clorazepate) |
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___ __ agents have favorable pharmacokinetic characteristics, and have relatively mild side effects that allow their use along with the more traditional anti-seizure meds |
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Definition
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Name the 3 factors associated with successful medication withdrawal |
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Definition
-Being free of seizures for at least 2 years while on meds -Having a normal neurologic examination prior to withdrawal -Being young when the seizures started |
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