Term
|
Definition
| Inhibits phosphodiesterase 5 thereby increasing cGMP resulting in vasodilation and erection. CNS stimulation and labido need to be intact in order for this medication to exert it's effect. Onset is 30-60 minutes and duration is 6 hours. ADR include flushing and headache. When taken with nitrates or alpha blockers, can increase hypotensive effects. |
|
|
Term
|
Definition
| A second-generation H1 antagonist used for allergies, hay-fever, and urticaria. Generally well tolerated. May cause sedation or arrhythmia in overdose. PO dosing. Available over the counter. |
|
|
Term
|
Definition
| A five HT1 agonist used for migraine headache suppression. Exact MOA is unknown but thought to cause vasoconstriction in large intracranial arteries. May cause tingling and warmth to fingers and chest. This medication is therefore contraindicated in those with a cardiac history. Use cautiously in those taking SSRI's or SNRI's as this may increase serotonin levels and increase the risk for serotonin syndrome. Sumatriptan is metabolized in the liver, so exercise caution in those with liver impairement. |
|
|
Term
|
Definition
| 5-HT3 antagonist- blocks type 3 serotonin receptrs on afferent vagal neurons in the upper gI tact. |
|
|
Term
|
Definition
| used to control nausea in post-op and chemo pts, no efficacy with motion sickness. Improved effecacy when combined with decadron.Investigation into use with ETOH abuse and cravings for ETOH. |
|
|
Term
|
Definition
| Do not use with long QT interval- can cause Torsades de Pointes. No EPS-like effects since it does not block dopamine. Pregnancy safe. |
|
|
Term
|
Definition
| Considered a first generation (meaning strong sedative effects) H1 antihistamine. It is a competitive antagonist/inverse antagonist at H1 receptors. |
|
|
Term
|
Definition
| Reduces or prevents histamine effects on smooth muscle and immune cells. It also blocks muscarinic and alpha-adrenoceptors. It is highly sedative. |
|
|
Term
|
Definition
| IgE immediate allergies, especially hay fever and urticaria. Often used as a seative, antiemetic, and anti-motion sickness drug. |
|
|
Term
| Adverse Effects of diphenhydramine |
|
Definition
| Sedation when used in hay fever, muscarinic blockade symptoms, and orthostatic hypotension. Can cause additive sedation when mixed with other sedatives, including alcohol. Some inhibition of CYP2D6 which may prolong the action of some beta-blockers. |
|
|
Term
|
Definition
| A process in which a drug induces/initiates/enhances the expression of an enzyme. The drug increases the activity by binding to enzyme and activating it or by increasing the expression of the gene coding. |
|
|
Term
|
Definition
| Examples- Buspirone a serotonin 5-HT1a agonist used to treat generalized anxiety . Triptans- selective agonists for serotonin 5HT1d and 5HT1b receptors used for treatment of migraine for the vasoconstriction properties. |
|
|
Term
|
Definition
The Adverse Event Reporting System (AERS) is a FDA database for reporting post marketing safety surveillance
events & errors for all drugs & biolgic products. Reporting Adverse events & med errors by healthcare professionals & consumers is voluntary & mandatory in the USA and the information is used to maintain or modify safety of products. Adverse events & med errors can also be reported to product manufacturer's and the manufacturer is required to report to the FDA. Medwatch Forms 3500 & 3500A can be accessed by computer on FDA website or paper form and reporting of an issue should occur within 15 days of event or error. Mandatory reporting is required for OTC & dietary supplements, drug/biologic/human cell; Tissues, Cellular & tissue based products manufacturer distributors,& packers, clinical trial events. Errors occuring in a medical facilty should be reported immediately to supervisor or manager & each medical facility has a paper or computerized form for reporting events & errors and is usually reviewed by the safety officer. Each form requires documented information such as demographics, incident, type of incident, where it occured, how & why it occured, what corrective action occured, and changes to prevent reoccurence. The goal is to improve or maintain safety issues for products and medications. |
|
|
Term
|
Definition
| 5-HT3 blockade in gut and CNS with shorter duration of binding than alosetron. |
|
|
Term
| Ondansetron Clinical Uses |
|
Definition
| Effective in preventing chemo induced and post operative N/V. |
|
|
Term
|
Definition
| HA, dizziness, constipation |
|
|
Term
| Types of enzyme inhibition |
|
Definition
| 1. Inhibit cytochrome P450 enzyme activity. 2. Irreversibly inhibit P450 by covalent interaction of a reactive intermediate. 3. Suicide inhibitor - inactivators that attack the heme or protein part of a molecule |
|
|
Term
| Drugs that inhibit cytochrome P450 activity |
|
Definition
| Cimetidine and ketoconazole reduce metabolism of testosterone. Macrolide antibiotics (troleandomycin, erythromycin) inactivate iron. |
|
|
Term
| Drug that irreversibly inhibits P450 |
|
Definition
| Chloramphenicol (antibiotic) |
|
|
Term
|
Definition
| Some steroids (ethinyl, estradiol, norethindrone, sprionolactone), fluroxene, allobarbital, analgesic sedatives (allylisopropylacetyl-urea, diethylpentenamide, ethchlorvynol), carbon disulfide, grapefruit, selegiline, phencyclidine, ticlopidine, clopidogrel, ritonavir, propylthiouracil |
|
|
Term
|
Definition
| When a drug causes the increased production of an enzyme or reduces the rate of degradation. The increase in the amount of enzymes can lead to an increase in the rate of drug metabolism. This can reduce the clinical effectiveness of medications because they will be more rapidly metabolised due to the increase in metabolizing enzymes. |
|
|
Term
|
Definition
| suppresses the activity of osteoclasts in part via the inhibition of farnesyl pyrophosphate synthesis |
|
|
Term
| Aldendronate Clinical Uses |
|
Definition
| osteoporosis, bone mets, hypercalcemia |
|
|
Term
| Aldendronate Pharmakinetics |
|
Definition
| daily or weekly dosing, effective in men & women |
|
|
Term
| Aldendronate Adverse Reactions |
|
Definition
| Adynamic bone, possibly renal failure, GI upset/ulcer - must stay up right 30 minutes after taking, rare femur fractures |
|
|
Term
|
Definition
| FDA approved for migraine and vascular (cluster) headaches |
|
|
Term
|
Definition
| A vasoselective ergot alkaloid. Ergotamine has a mixed partial agonist effect at 5-HT2 and α adrenoceptors. Causes marked smooth muscle contraction but blocks α-agonist vasoconstriction. |
|
|
Term
|
Definition
Serious side effects of Ergotamine include:
• Disorder of cardiovascular system, Angina, MI, arrhythmia
• Ergotism, Vasoconstriction, vascular spasm, cyanosis, numbness of the extremities, possible gangrene
• Retroperitoneal fibrosis |
|
|
Term
|
Definition
| partial agonist at 5-HT1D/1B receptors, possibly reducing the release of calcitonin gene-related peptide and perivascular edema in cerebral circulation (MOA/effects not fully understood) |
|
|
Term
| Sumatriptan Clinical Uses |
|
Definition
| Migraine & Cluster headaches |
|
|
Term
|
Definition
| paresthesias, dizziness, muscle weakness, neck pain, coronary vasoconstriction/vasospasm |
|
|
Term
| loratadine (Claritin) MOA |
|
Definition
| second generation H1 blocker: competitive antagonism/inverse agonism at H1 receptors |
|
|
Term
|
Definition
| reduces or prevents histamine effects on smooth muscle, and immune cells |
|
|
Term
|
Definition
| allergic reaction IgE immediate allergies, hay fever , allergic rhinitis, urticaria, can be found OTC |
|
|
Term
| Loratidine S/E and Toxicities |
|
Definition
| Toxicities: sedation and arrhythmias with overdose, S/E: nonsedative unlike 1st generation H1 antagonists |
|
|
Term
|
Definition
| First generation H1 antagonist: competitive antagonis/inverse agonism at H1 receptors |
|
|
Term
|
Definition
Reduces or prevents the action of histamine by reversible competitive binding to the H1 receptor. Reduces histamine effects on smooth muscles, immune cells.
Also blocks muscarinic and alpha adrenoceptors, highly sedative
First drugs sed to prevent or treat symptoms of allergic reactions. |
|
|
Term
| Diphenhydramine Clinical Use |
|
Definition
IgE immediate allergie, especially hay fever, uticaria
Often sed as a sedative, antiemetic, and anti-motion sickness drug
Has acute suppressant effects on the extrapyramidal symptoms associated with certain antipsychotic drugs, antiparkinsonism effects
Used as local anesthesia by blocking sodium channels in excitable membranes |
|
|
Term
|
Definition
| Sedation, muscarinic blockade symptoms, orthostatic hypotension |
|
|
Term
|
Definition
| Inhibits phosphodiesterase isoform 5 (PDE) which inhibits the breakdown of cGMP. This increase in cGMP leads to vasoldilation and erection. |
|
|
Term
| Sildenafil Pharmacokinetics |
|
Definition
| Onset of action is 30-60 minutes; Duration 6 hours; Use the lowest effective dose to minimize hypotension and flushing. Must have CNS stimulation and an intact libido. |
|
|
Term
|
Definition
| Flushing, headache, visual disturbances; effect color vision causing difficulty in blue-green discrimination |
|
|
Term
| Sildenafil Drug Interactions |
|
Definition
| Interacts with nitrates (seperate dose by 6 hours) and alpha blockers |
|
|
Term
| Diphenhydramine (Clinical Uses) |
|
Definition
Hypersensitivity reactions; Allergic rhinitis; Anaphylaxis;
Adjunct;Common cold; Insomnia; Motion
sickness; Parkinsonism; Pruritus
of skin |
|
|
Term
|
Definition
| Binds to central and peripheral H1 receptors by competing with histamine for receptor sites on effector cells' by blocking histamine it produces antihistamine effects, inhibiting repiratory, vascular, and GI smooth-muscle contractions; decreasing capillary permeability, which reduces wheals, flares, and itching |
|
|
Term
|
Definition
| Xerostomia, Dizziness, drowsiness, Dyskinesia, Sedated; Somnolence; Nasal mucosa dry, Pharyngeal dryness, Thick sputum, Bronchial |
|
|
Term
|
Definition
| Is an alpha adrenergic antagonist drug with partial agonist effect at the 5-HT2 receptors to produce smooth muscle contraction. It does block vasoconstriction at the alpha adrenoreceptor sites. Its highly effective for migraine or cluster headache pain because of its contraction of smooth muscles in the vasculature in the cranium. It also produces smooth muscle contraction in the periphery vasculature. |
|
|
Term
|
Definition
| Mild: GI disturbances (nasuea, vomting), weakness, visual disturbance. LIFE Threatening: prolonged vasospasm leading to angina, gangrene or uterine spasms |
|
|
Term
|
Definition
Bisphosphonate class that prevents bone resorption by:
--Inhibiting osteoCLAST recruitment
--Inducing osteoCLAST apoptosis
--Stimulating osteoBLAST activity |
|
|
Term
|
Definition
| GI upset, ulceration, bone pain |
|
|
Term
| Alendronate special circumstances |
|
Definition
--Special administration requirements:
Full glass of water
Empty Stomach
Upright 30 minutes after admin |
|
|
Term
|
Definition
| Causes an increase in the metabolism of a drug |
|
|
Term
|
Definition
| Reporting an adverse drug reaction can be done online, by phone, or by submitting the MedWatch 3500 form by mail or fax. |
|
|
Term
|
Definition
| Report ADR online: http://www.fda.gov/Safety/MedWatch/HowToReport/default.htm |
|
|
Term
| Reporting an ADR by phone |
|
Definition
| Call 1-800-FDA-1088 to report by telephone |
|
|
Term
| Reporting and ADR via mail or fax |
|
Definition
| Download MedWatch 3500 form or call 1-800-332-1088 to request a reporting form, then complete and return to the address on the pre-addressed form, or submit by fax to 1-800-FDA-0178. MedWatch form found at: https://www.accessdata.fda.gov/scripts/medwatch/medwatch-online.htm |
|
|
Term
|
Definition
| Inhibits cytochrome P450 enzyme activity to reduce metabolism of certain drug |
|
|
Term
|
Definition
| Irreversible enzyme inhibition |
|
|
Term
| Ondansetron (Zofran) pharmacologic category |
|
Definition
| Selective 5-HT3 receptor antagonist; antiemetic |
|
|
Term
|
Definition
| Selective 5-HT3-receptor antagonist that blocks serotonin. Occurs mainly instestinal and peripheral vagal nerve terminals, also centrally in the vomiting center and chemoreceptor trigger zone (CTZ) |
|
|
Term
| Clinical usees of Ondansetron |
|
Definition
| Vagal stimulated N/V, post-op N/V, chemotherapy-induced N/V (unlabeled use: hyperemesis gravidarum) |
|
|
Term
| Ondansetron may be administered by which route(s)? |
|
Definition
|
|
Term
|
Definition
| HA, dizziness, constipation, small QT prolongation. Very well tolerated |
|
|
Term
|
Definition
| Some hepatic metabolism by P450 but no significant drug interactions. Half-life: 4-9 hrs |
|
|
Term
| Ondansetron pregnancy category |
|
Definition
|
|
Term
| Sildenafil (Viagra) Class |
|
Definition
Antihypertensive, Peripheral Vasodilator
Erectile Dysfunction Agent
Phosphodiesterase Type 5 Inhibitor
Vasodilator |
|
|
Term
| Sildenafil FDA approved indications |
|
Definition
| Erectile dysfunction & Pulmonary HTN |
|
|
Term
|
Definition
* Acts to increase cGMP by inhibiting its breakdown by phosphodiesterase isoform 5 (PDE-5).
* Increases cGMP within vascular smooth muscle cells resulting in relaxation and vasodilation.
* In patients with pulmonary HTN - leads to vasodilation of the pulmonary vascular bed.
* In patients with erectile dysfunction, sildenafil citrate enhances the effect of nitric oxide (NO) by inhibiting PDE5 in the corpus cavernosum. |
|
|
Term
| Sildenafil (Viagra) Considerations |
|
Definition
* Approved for use in pulomonary arterial hypertension.
* Little or no value in men with loss of potency due to cord injury or other damage to innervation and in men lacking libido.
* Potentiates the action of nitrates used for angina, and severe hypotension and a few myocardial infarctions have been reported in men taking both drugs. It is recommended that at least 6 hours pass between use of a nitrate and the injestion of sildenafil.
* Has effects on color vision, causing difficulty in blue-green discrimination. |
|
|
Term
| Sildenafil (Viagra) dosage/effects |
|
Definition
| 25 to 100 mg (50 mg usual dose) orally 1 hour (range 0.5 to 4 hours) prior to sexual activity; MAX frequency of administration once daily |
|
|
Term
|
Definition
| Cardiovascular morbidity, Decreased hearing (sudden onset), myocardial infarction, non-arteritic ischemic optic neuropathy, priapism, prolonged erection of penis, retinal hemorrhage, sickle cell anemia with vasoocclusive crisis and sudden hearing loss |
|
|
Term
|
Definition
| 2nd generation antihistamine; H1 blocker |
|
|
Term
|
Definition
|
|
Term
| Loratadine drug interactions |
|
Definition
| minimal- do not have CPY 450 enzymes problems with drug interactions that other 2nd generation do with macrolides and antifungal azoles |
|
|
Term
|
Definition
| competitive antagonism/ inverse agonism @ H1 receptors- reduce or prevent histamine effect on smooth muscle & immune cells |
|
|
Term
| Loratadine clinical applications |
|
Definition
| IgE immediate allergies, especially hay fever (allergic rhinitis), most effective in anticipation; chronic urticaria |
|
|
Term
|
Definition
| PO; longer durations than 1st generation (12-24 hrs); rapidly absorbed; peak 1-2 hrs; widely distributed but does not cross BBB; active metabolite is desloratadine; most effective when administered before histamine release |
|
|
Term
| loratadine ADR & toxicity |
|
Definition
| little to no sedative or stimulant actions & fewer autonomic effects than 1st generation; sedation & arrhythmias in overdose |
|
|
Term
| Diphenhydramine Classification |
|
Definition
| Antihistamine (1st generation, non selective), Ethanolamine Derivative, H1-receptor antonist |
|
|
Term
|
Definition
| Acts on blood vessels, GI, respiratory sytem by competing with histamine for H1-receptor site; decreases the allergic response by blocking histamine |
|
|
Term
|
Definition
| Allergy symptoms, rhinitis, motion sickness, antiparkinsonism, night time sedation, infant colic, nonproductive cough, insominia in children. |
|
|
Term
| Diphenhydramine Contraindications |
|
Definition
| Pregnancy category B, hypersensitivity to H1-receptor antagonist, acute asthma attack, lower respiratory disease. |
|
|
Term
|
Definition
| Dizziness, drowsiness, seizures, urinary retention, anxiety, fatigue, poor corrdination, dry nose, nasal stuffiness, blurred vision. |
|
|
Term
| Diphenhydramine Pharmacokinetics |
|
Definition
| Metabolized in the liver, excreted in the kidneys, crosses the placenta and is exreted in breast milk |
|
|
Term
| Diphenhydramine Half-life / kinetics |
|
Definition
| Half-life = 2-7 hrs, PO (peak 1-3 hrs, duration 4-7 hrs), IM (onset 30 min, peak 1-4 hrs, duration 4-7 hrs). |
|
|
Term
| Diphenhydramine Interactions |
|
Definition
| CNS depression - barbiturates, opiates, hypnotics, tricyclics, ETOH, Increases the effects of MAOI's |
|
|
Term
| Sumatriptan (Imitrex) Pharmacologic Classification |
|
Definition
| 5-HT 1B/1D serotonin agonist |
|
|
Term
|
Definition
| Effects not fully understood, but 2 proposed theories involve inhibiting the release of vasodilating pepties and prevent vasodilation and stretching of pain endings |
|
|
Term
| Sumatriptan Clinical Uses |
|
Definition
| First line of therapy for acute, severe migraine attacks |
|
|
Term
| Sumatriptan Pharmacokinetics |
|
Definition
| Duration is 2 hours, half life is 2 hours. Sometimes multiple doses may need to be given, other triptans have longer duration but more expensive and have more negative interactions |
|
|
Term
|
Definition
| Tingling, warmth, dizziness, vasoconstriction |
|
|
Term
|
Definition
| Additive with other vasoconstrictors, should not be given to patients with CAD |
|
|
Term
|
Definition
| Refers to the way a drug can cause increased expression of an enzyme leading to an enhanced rate of synthesis, or reduced rate of degredation of the drug metabolism |
|
|
Term
|
Definition
| Molecule which binds to enzymes and decreases their activity, metabolism and/or inhibits the enzymes. For example, Macrolide antibiotics such as troleandomycin, erythromycin and erythromycin derivatives are metabolized by CYP3A to metabolites that complex the cytochrome P450 heme iron and render it catalytically inactive. See table 4-2 (P.58) for more example of inhibitors. |
|
|
Term
| What produces enzyme inhibition in statins? |
|
Definition
| Drugs that inhibit the metabolism of CYP3A4 (ex- erythromycin) place the patient at an increased risk for toxicity from simvastatin. |
|
|
Term
| What produces enzymatic inhibition in clopidogrel? |
|
Definition
| Clopidogrel must be converted to its active form by CYP2C19. Inhibitors like sertraline and omeprazole decrease its antiplatelet activity |
|
|
Term
| What produces enzymatic inhibition in tamoxifen? |
|
Definition
| Tamoxifen is a pro-drug. Paroxetine inhibits CYP2D6 that converts tamoxifen to its active form. This causes more cancer deaths in patient on tamoxifen to prevent breast cancer. |
|
|
Term
| Define an Adverse Drug Reaction: |
|
Definition
| a harmful or unintended response to a drug |
|
|
Term
| Deaths from Adverse Drug Reactions are the ____________ leading cause of death in this country. |
|
Definition
|
|
Term
| Where/how do Healthcare providers report Adverse Drug Reactions? |
|
Definition
* The FDA-sponsored Med Watch program collects data on safety and adverse drug effects.
* Healthcare professionals, consumers, and patients fall under Voluntary reporting requirements.
* The Online Voluntary Reporting form is available at: https://www.accessdata.fda.gov/scripts/medwatch/medwatch-online.htm |
|
|
Term
| Ondansetron (Zofran) pharmacologic category |
|
Definition
| Selective 5-HT3 receptor antagonist; antiemetic |
|
|
Term
|
Definition
| Selective 5-HT3-receptor antagonist that blocks serotonin. Occurs mainly instestinal and peripheral vagal nerve terminals, also centrally in the vomiting center and chemoreceptor trigger zone (CTZ) |
|
|
Term
| Clinical usees of Ondansetron |
|
Definition
| Vagal stimulated N/V, post-op N/V, chemotherapy-induced N/V (unlabeled use: hyperemesis gravidarum) |
|
|
Term
| Ondansetron may be administered by which route(s)? |
|
Definition
|
|
Term
|
Definition
| HA, dizziness, constipation, small QT prolongation. Very well tolerated |
|
|
Term
|
Definition
| Some hepatic metabolism by P450 but no significant drug interactions. Half-life: 4-9 hrs |
|
|
Term
| Ondansetron pregnancy category |
|
Definition
|
|
Term
| Sildenafil (Viagra) Class |
|
Definition
Antihypertensive, Peripheral Vasodilator
Erectile Dysfunction Agent
Phosphodiesterase Type 5 Inhibitor
Vasodilator |
|
|
Term
| Sildenafil FDA approved indications |
|
Definition
| Erectile dysfunction & Pulmonary HTN |
|
|
Term
|
Definition
* Acts to increase cGMP by inhibiting its breakdown by phosphodiesterase isoform 5 (PDE-5).
* Increases cGMP within vascular smooth muscle cells resulting in relaxation and vasodilation.
* In patients with pulmonary HTN - leads to vasodilation of the pulmonary vascular bed.
* In patients with erectile dysfunction, sildenafil citrate enhances the effect of nitric oxide (NO) by inhibiting PDE5 in the corpus cavernosum. |
|
|
Term
| Sildenafil (Viagra) Considerations |
|
Definition
* Approved for use in pulomonary arterial hypertension.
* Little or no value in men with loss of potency due to cord injury or other damage to innervation and in men lacking libido.
* Potentiates the action of nitrates used for angina, and severe hypotension and a few myocardial infarctions have been reported in men taking both drugs. It is recommended that at least 6 hours pass between use of a nitrate and the injestion of sildenafil.
* Has effects on color vision, causing difficulty in blue-green discrimination. |
|
|
Term
| Sildenafil (Viagra) dosage/effects |
|
Definition
| 25 to 100 mg (50 mg usual dose) orally 1 hour (range 0.5 to 4 hours) prior to sexual activity; MAX frequency of administration once daily |
|
|
Term
|
Definition
| Cardiovascular morbidity, Decreased hearing (sudden onset), myocardial infarction, non-arteritic ischemic optic neuropathy, priapism, prolonged erection of penis, retinal hemorrhage, sickle cell anemia with vasoocclusive crisis and sudden hearing loss |
|
|
Term
|
Definition
| 2nd generation antihistamine; H1 blocker |
|
|
Term
|
Definition
|
|
Term
| Loratadine drug interactions |
|
Definition
| minimal- do not have CPY 450 enzymes problems with drug interactions that other 2nd generation do with macrolides and antifungal azoles |
|
|
Term
|
Definition
| competitive antagonism/ inverse agonism @ H1 receptors- reduce or prevent histamine effect on smooth muscle & immune cells |
|
|
Term
| Loratadine clinical applications |
|
Definition
| IgE immediate allergies, especially hay fever (allergic rhinitis), most effective in anticipation; chronic urticaria |
|
|
Term
|
Definition
| PO; longer durations than 1st generation (12-24 hrs); rapidly absorbed; peak 1-2 hrs; widely distributed but does not cross BBB; active metabolite is desloratadine; most effective when administered before histamine release |
|
|
Term
| loratadine ADR & toxicity |
|
Definition
| little to no sedative or stimulant actions & fewer autonomic effects than 1st generation; sedation & arrhythmias in overdose |
|
|
Term
| Diphenhydramine Classification |
|
Definition
| Antihistamine (1st generation, non selective), Ethanolamine Derivative, H1-receptor antonist |
|
|
Term
|
Definition
| Acts on blood vessels, GI, respiratory sytem by competing with histamine for H1-receptor site; decreases the allergic response by blocking histamine |
|
|
Term
|
Definition
| Allergy symptoms, rhinitis, motion sickness, antiparkinsonism, night time sedation, infant colic, nonproductive cough, insominia in children. |
|
|
Term
| Diphenhydramine Contraindications |
|
Definition
| Pregnancy category B, hypersensitivity to H1-receptor antagonist, acute asthma attack, lower respiratory disease. |
|
|
Term
|
Definition
| Dizziness, drowsiness, seizures, urinary retention, anxiety, fatigue, poor corrdination, dry nose, nasal stuffiness, blurred vision. |
|
|
Term
| Diphenhydramine Pharmacokinetics |
|
Definition
| Metabolized in the liver, excreted in the kidneys, crosses the placenta and is exreted in breast milk |
|
|
Term
| Diphenhydramine Half-life / kinetics |
|
Definition
| Half-life = 2-7 hrs, PO (peak 1-3 hrs, duration 4-7 hrs), IM (onset 30 min, peak 1-4 hrs, duration 4-7 hrs). |
|
|
Term
| Diphenhydramine Interactions |
|
Definition
| CNS depression - barbiturates, opiates, hypnotics, tricyclics, ETOH, Increases the effects of MAOI's |
|
|
Term
| Sumatriptan (Imitrex) Pharmacologic Classification |
|
Definition
| 5-HT 1B/1D serotonin agonist |
|
|
Term
|
Definition
| Effects not fully understood, but 2 proposed theories involve inhibiting the release of vasodilating pepties and prevent vasodilation and stretching of pain endings |
|
|
Term
| Sumatriptan Clinical Uses |
|
Definition
| First line of therapy for acute, severe migraine attacks |
|
|
Term
| Sumatriptan Pharmacokinetics |
|
Definition
| Duration is 2 hours, half life is 2 hours. Sometimes multiple doses may need to be given, other triptans have longer duration but more expensive and have more negative interactions |
|
|
Term
|
Definition
| Tingling, warmth, dizziness, vasoconstriction |
|
|
Term
|
Definition
| Additive with other vasoconstrictors, should not be given to patients with CAD |
|
|
Term
|
Definition
| Refers to the way a drug can cause increased expression of an enzyme leading to an enhanced rate of synthesis, or reduced rate of degredation of the drug metabolism |
|
|
Term
|
Definition
| Molecule which binds to enzymes and decreases their activity, metabolism and/or inhibits the enzymes. For example, Macrolide antibiotics such as troleandomycin, erythromycin and erythromycin derivatives are metabolized by CYP3A to metabolites that complex the cytochrome P450 heme iron and render it catalytically inactive. See table 4-2 (P.58) for more example of inhibitors. |
|
|
Term
| What produces enzyme inhibition in statins? |
|
Definition
| Drugs that inhibit the metabolism of CYP3A4 (ex- erythromycin) place the patient at an increased risk for toxicity from simvastatin. |
|
|
Term
| What produces enzymatic inhibition in clopidogrel? |
|
Definition
| Clopidogrel must be converted to its active form by CYP2C19. Inhibitors like sertraline and omeprazole decrease its antiplatelet activity |
|
|
Term
| What produces enzymatic inhibition in tamoxifen? |
|
Definition
| Tamoxifen is a pro-drug. Paroxetine inhibits CYP2D6 that converts tamoxifen to its active form. This causes more cancer deaths in patient on tamoxifen to prevent breast cancer. |
|
|
Term
| Define an Adverse Drug Reaction: |
|
Definition
| a harmful or unintended response to a drug |
|
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Term
| Deaths from Adverse Drug Reactions are the ____________ leading cause of death in this country. |
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Definition
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Term
| Where/how do Healthcare providers report Adverse Drug Reactions? |
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Definition
* The FDA-sponsored Med Watch program collects data on safety and adverse drug effects.
* Healthcare professionals, consumers, and patients fall under Voluntary reporting requirements.
* The Online Voluntary Reporting form is available at: https://www.accessdata.fda.gov/scripts/medwatch/medwatch-online.htm |
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