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123 Cards in this Set
- Front
- Back
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Carbon Monoxide
[Air Pollutant] |
*Leading cause of death by poisoning
- *can inflict "sublethal injuries" = MI and cerebral atrophy 52% of air pollution - can occur from auto exhaust system leaks and inadequate heater ventilation - displaces O2 from Hgb due to its 200-fold greater binding affinity, and once attached the Hbg cannot transport O2 - smokers have 5-10% carboxyhemoglobin and those who collapse have 40-60% - S/Sx = nervous system dysfunction similar to the flu, then depressed sensory function, then LOC, seizure, death - remove from exposure, maintain resp, administer O2 |
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Sulfur Dioxide
[Air Pollutant] |
Colorless irritant gas formed via fossil fuel combustion
- SO2 forms sulfurous acid - S/Sx = irritation of eyes/mucous membranes/skin, bronchoconstriction, altered smooth muscle tone and parasympathetic reflexes - severe exposure may lead to delayed onset pulmonary edema - remove from exposure, maintain resp, administer O2 |
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Nitrogen Oxide
[Air Pollutant] |
Brownish irritant gas sometimes associated with fires
- *stay out of silos - formed from fresh silage and can lead to silo-filler's disease - deep lung irritant; can produce pulmonary edema - S/Sx = irritation of eyes/nose, cough, mucoid or frothy sputum production, dyspnea and pain; recurring pulmonary edema and fibriotic destruction of terminal bronchiole |
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***Lead***
[Heavy Metal] |
present in paints, ceramic glazes, lead mining and various work environments
- binds to sulfur atoms leading to deactivation of many enzymes - toxic to nervous system with age specific signs and symptoms - S/Sx = Children present with anorexia, colicky abdominal pain, lethargy and vomiting; Adults present with encephalopathy, irritability, seizures and coma (30% permanent neurological sequelae) - manage with chelation and supportive care |
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Chlorophenoxy Herbicides
[Herbicide] |
2,4-D is used to destroy weeds and in large doses can cause coma and muscle hypotonia
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Bipyridyl Herbicides
[Herbicide] |
Paraquat is an agent that slowly accumulates in the lung causing edema, alveolitis and progressive fibrosis
- S/Sx after oral exposure = GI irritation (hematemesis and bloody stools) followed by respiratory distress - interval between ingestion and death may be several weeks - manage via gastric lavage, cathartics, adsorbents and supportive O2 |
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Polychlorinated Biphenyls [PCBs]
[Environmental Pollutant] |
used in dielectric and heat transfer fluids
- S/Sx = chloracne, folliculitis, erythema, dryness, and rash |
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Dioxin
[Environmental Pollutant] |
dibenzo-p-dioxin and tetrachlorodibenzo-p-dioxin are unwanted byproducts of PCBs that contaminate a variety of products
- stable and persist in environment - S/Sx = wasting, epidermal changes, immunotoxicity, atrophy, hepatotoxicity, effects of development and reproduction |
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Benzocaine
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Can cause methoemoglobinemia
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*Cimetidine [---tidine]
(Tagamet) [GI Drug] |
H2 receptor antagonist/blocker
competitively inhibit H2 receptors --> decrease cAMP --> less acid secreted - well absorbed - may cause diarrhea, N/V, mental confusion, gynecomastia - inhibits cytochrome P450, many drug interactions - first one to be introduced and is now an OTC |
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*Misoprostol
(Cytotec) [GI Drug] |
for NSAID-induced ulcers; synthetic PG
- increases bicarbonate release, neutralizes acid; binds prostaglandin receptor, decreases cAMP and decreases proton pump and gastric acid secretion - PO, easily absorbed - effective in reducing mucosal damage from chronic use of NSAIDs - may cause abdominal pain, diarrhea, and uterine contractions which can lead to miscarriages and abortions |
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*Omeprazole [---prazole]
(Prilosec) [GI Drug] |
irreversibly inhibits H/K dependent ATPase proton pump --> decrease in acid secretion
- increases concentrations of other drugs - effective for Zollinger-Ellison syndrome pts (gastrin-secreting tumor) and ulcer pts who are resistant to H2-receptor blockers - inhibits P450 |
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Calcium Carbonate
(Tums) [antacid; GI Drug] |
weak base neutralized gastric acid
- can cause hypercalcemia and cardiac arrhythmia - less soluble - non-systemic, longer duration of aaction - treats duodenal ulcers |
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*Sucralfate
(Carafate) [mucosal protective agent; GI Drug] |
covers the gastric surface or stimulates mucous secretion
- may cause constipation - sucrose complex - aluminum hydroxide sulfate |
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*Colloidal Bismuth
(deNol, Pepto Bismol) [mucosal protective agent; GI Drug] |
binds and coats ulcer tissues
- anti-diarrheal activity - produces black tongue and black stools |
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**Metoclopramide
(Reglan) [Prokinetic drug; GI Drug] |
antagonizes dopamine receptor --> increase LES tone and increase in gastric emptying
- may cause fatigue, insomnia, and altered motor coordination -also an anti-emetic by binding to CTZ in medulla - treat constipation |
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*Cisapride
(Propulsid) [Prokinetic drug] |
stimulates 5HT3 receptor --> increase Ach release --> increase in gastric motility
- not anti-dopaminergic - may cause diarrhea and general cholinergic effects - treat constipation |
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**Ondansetron (Zofran)
[anti-emetic] |
5HT3 receptor blockers/serotonin antagonist --> blocks CTZ --> prevents stimulation of vomiting center
- may cause constipation, diarrhea, dizziness, urinary retention - most effective; #1 |
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*Prochlorperazine (Compazine)
[anti-emetic] |
dopamine antagonist; blocks receptors of CTZ in medulla --> prevents stimulation of vomiting center
- discontinued in US |
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Prometazine (Phernergan)
[anti-emetic] |
dopamine antagonist; blocks receptors of CTZ in medulla --> prevents stimulation of vomiting center
- may cause drowsiness, sedation, dizziness, confusion, dry mouth, respiratory depression, gangrene if injected |
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Scopolamine
[anti-emetic] |
anti-muscarinic drug/blocks muscarinic receptors
- given as a patch prophylactically for motion sickness - anticholinergic effects such as dry mouth, urine retention, tachycardia, vision problems, etc |
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**Loperamide HCl
(Imodium) [opiate like anti-diarrheal] |
dehydrates feces; increase segmentation and decrease rate of propulsive movement/peristalsis
- may cause constipation, respiratory depression and addiction - do not leave GI tract |
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Sulfasalazine
(Azulfidine) [treat IBD] |
local anti-inflammatory
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Infliximab
(Remicade) [treat IBD] |
monoclonal antibody that targets TNF-alpha --> decrease inflammation
= anti-TNF |
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Chenodiol
(Chenix) [treat gallstones] |
naturally occurring bile acids that dissolve stones if they are made of cholesterol
- PO; takes months to work |
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Methyltertriary-butyl ether
(MTBE) [treat gallstones] |
organic solvent that dissolves stones
- given locally via catheter; dissolves in hours |
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Sildenafil
(Viagra) [ED treatment] |
- potent PDE5 inhibitor so increase in cGMP
- augments the effects of intracorporal cGMP - only works under condition of sexual stimulation - rapidly absorbed, onset of action = 1 hour normal duration 4 hr - due to high plasma conc, erections can be achieved for up to 36 hrs but only works for 65-70% of patients **SE: headache, flushing, nasal stuffiness, dysphagia/dyspepsia, blue aura (effect of PDE6), priapsim (serious, ER) (aspirate to treat) off label use for viagra = pulmonary HTN or high altitude pulmonary edema |
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Vardenafil
(Levitra) [ED treatment] |
PDE5 inhibitor
onset 30 min, 24 hour duration **SE: headache, flushing, **rhinitis |
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Tadalafil
(Cialis) [ED treatment] |
PDE5 inhibitor
onset 30 min, 36 hour duration **SE: headache, dysphagia, **backache and muscle ache Off label use for high-altitude pulmonary edema |
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**L-DOPA/Levodopa +
Carbodopa = (Sinemet) [PD treatment] |
dopamine replacement; Prodrug for dopamine
- L-dopa is a metabolic precursor of dopamine which can cross the BBB - Carbidopa is a dopamine decarboxylase inhibitor but stays in the periphery - when used together, more levodopa ends up in brain and get less SE - take before or after meals - absorbed from SI by active transport for aromatic amino acids, short half life - sodium dependent carrier for transport into CNS - SE: N/V, arrhythmias and hypotension, invol movements can occur with long term therapy; mood changes and depression may occur drug interactions: pyridoxine and carbidopa bind to same site on decarboxylase enzyme so can reduce effectiveness of carbidopa and enhance extracerebral metabolism of L-DOPA (found in many multivitamins) - on/off phenomenon where there are fluctuations in motor response that cause pt to suddenly lose normal mobility and exp tremors, cramps and immobility (most likely due to loss of remaining dopamine neurons, less storage and less buffering capacity of concentrations as levodopa enters brain |
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Amantadine
(Symmetrel) [PD treatment] |
enhance synthesis, release, or re-uptake of dopamine form surviving nigral neurons (only uselful early on)
SE: restlessness, agitation, confusion, hallucinations orthostatic hypotension, urinary retention, peri edema, dry mouth may occur |
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*Bromocriptine
(Parlodel) [PD treatment] |
ergotamine derivative dopamine agonist
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*Benztropine
(Cogentin) [PD treatment] |
Anticholinergic (not preferred)
SE: memory loss, dry mouth, decreased sweating, constipation, impaired bladder |
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*Donepezil
(Aricept) [treat Alzheimer's] |
Cholinesterase/acetylcholine esterase inhibitor
- good bioavailability, #1 drug - lipophilic so can cross membrane to go into CNS - results in increased ACh - SE: general cholinergic effects: bradycardia, decreased CO, hypotension, bronchoconstriction, N/V/D, cramps, sweating, salivation, urinary urgency |
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*Memantine
(Namenda) [treat Alzheimer's] |
Glutamate antagonist; NMDA-receptor anatagonist
- decrease excitation and postpone loss of neurons via glutamate blockers |
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Fluoxetine (Prozac)
Paroxetine (Paxil) Escitalopram (Lexapro) [anti-depressants] |
SSRI - block reuptake of 5-HT serotonin
- not anticholinergic and safer in overdose - safer in cardiac patients - hydrophobic and readily enter CNS SE - anxiety, HA, N/D, insomnia, *sexual dysfunction the GI tract has lots of serotinin and serotonin receptors |
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Amitriptyline (Elavil)
Imipramine (Depranil) [anti-depressants] |
Tricyclics - block reuptake of serotonin, NE, dopamine
- SE: dry mouth, dry eyes, constipation, urinary retention (muscarinic blocker), sedation (histamine blocker), orthostatic hypotension (alpha blocker), sexual dysfunction, wt gain - contraindicated in pts with heart disease (increases arrhythmias) and epilepsy (lowered seizure threshold) - amitriptyline is an active compound and also blocks sodium channels and helps with neuropathic pain (altered membrane potential) - introduce birth of new neurons - lethal in OD |
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Venlafaxin (Effexor)
Duloxetine (Cymbalta) [anti-depressants] |
SNRI - serotonin-NE reuptake inhibitors
- little affinity for muscarinic, histamine or alpha receptors - SE: may increase BP, sexual dysfunction |
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Bupropion
(Wellbutrin) [anti-depressants] |
Dopamine-NE reuptake inhibitors
- SE: sedation, weight gain, and sexual dysfunction = alll RARE - there is a risk of seizure at higher doses - initially can be associated with anxiety and agitation - also a smoking cessation aid |
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Lithium
[bipolar treatment] |
mood-stabilizing - used to treat acute mania
- can substitute for Na in generating AP. At therapeutic concetrations, does not alter Na/K ATPase activity - appears to enhance actions of 5-HT - appears to block development of DA receptor supersensitivity - usually given as Lithium carbonate -disrupts electrochemical gradients across cell membrane - action on IP3 pathway; inositol from periphery does not cross BBB; Lithium depletes inositol in CNS - inhibits adrenergic, muscrinic, and serotonergic systems of CNS - SE: kidney and thyroid, therapeutic window very small; thirst, nausea, diarrhea, tremor, polyuria; chronic - diabetes insipidus via inhibition of vasopression action in kidney) - >2 plasma level leads to intoxication, seizures, coma and death 1.5-2 plasma level get NVD. tremors, ataxia |
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Chlorpromazine/Haloperidol
[typical antipsychotics] |
- block dopamine receptors only
- not used first, use 2nd generation and if it doesnt work, then come back to 1st generation - treats + sx but leads to many SE |
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Clozapine/Risperidone
[atypical antipsychotics] 2nd generation |
(mainstream 1st line tx); serotonin-dopamine antagonists
- block dopamine and serotinin receptors - fewer SE - serotonin inhibits DA release in nigrostriatal pathway and atypical antipsy exploit this ability of serotonin antagonist to offset D2 antagnosism --> DA release - therefore less extrapyramidal SE*** - therefore treat + and - sx - in mesocortical pathway, more serotonin receptors than D2 --> release of DA - in tuberoinfundibular pathway, serotonin stimulates prolactin release; serotonin antagonisms may reverse D2 antagonism - can cause diabetes/hyperglycemia |
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Morphine
[opiates] |
opiate receptor agonist
activates mu receptor; prototype - analgesia properties, decrease gastric motility, histamine release, feelings of detachment, decreased testosterone, smooth muscle spasm, urinary retention, respiratory depression, miosis, emesis |
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Fentanyl
[opiates] |
opiate receptor agonist
more potent - analgesia properties, decrease gastric motility, histamine release, feelings of detachment, decreased testosterone, smooth muscle spasm, urinary retention, respiratory depression, miosis, emesis |
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Methadone
[opiates] |
opiate receptor agonist
longer lasting - analgesia properties, decrease gastric motility, histamine release, feelings of detachment, decreased testosterone, smooth muscle spasm, urinary retention, respiratory depression, miosis, emesis used to prevent physical withdrawal sx |
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Heroin
[opiates] |
opiate receptor agonist
metabolized to morphine in the brain - analgesia properties, decrease gastric motility, histamine release, feelings of detachment, decreased testosterone, smooth muscle spasm, urinary retention, respiratory depression, miosis, emesis |
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Codeine
[opiates] |
opiate receptor agonist
orally active; less potent than morphine - cough suppressant - analgesia properties, decrease gastric motility, histamine release, feelings of detachment, decreased testosterone, smooth muscle spasm, urinary retention, respiratory depression, miosis, emesis |
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*Pentazocine
[opiates] |
Opiate receptor Agonist or Antagonist
- acts as an agonist in absence of other opiates, but an antagonist in presence of other opiates - agonist at kappa receptors and weak antagonist at mu receptors - will cause withdrawal in an addict |
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Naloxone
[opiates] |
Opiate receptor Antagonist
-***used to treat overdoses of opiates - will put an addict in immediate withdrawal |
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Naltrexone
[opiates] |
Opiate receptor Antagonist
- manage of alcohol and opiod dependence - will put an addict in immediate withdrawal |
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Dextromethorphan
[opiates] |
Mu agonists
cough suppressant, no analgesic action |
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Indomethacin
[NSAID] |
Tx of mild attack migraine
reversible, inhibits COX, less PG are made - for inflammation, pain and fever - can also be used to treat acute gout SE - GI bleeding, prolonged bleeding time |
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Aspirin
[NSAID] |
Tx of mild attack migraine
irreversible inhibitor of COX, less PGs made not to be used on young children with viral fever - for inflammation, pain and fever |
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Acetaminophen
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Tx of mild attack migraine
enters CNS. inhibits both COX1 and COX2, less PGs made safer in kids can be used for fever and pain only |
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Ibuprofen
[NSAID] |
Tx of mild attack migraine
reversible, inhibits COX, less PG are made - for inflammation, pain and fever |
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Naproxen
[NSAID] |
Tx of mild attack migraine
reversible |
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Sumatriptan (-triptan)
(Imetrex) [Migraine] |
tx for more severe migraine
- 5HT receptor agonist SE: tingling, paresthesias, snesations of warmth in neck, head, chest and limbs, sometimes dizziness, flushing, neck pain or stiffness. Rarely MI (some receptors found in coronary circulation) |
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Sevoflurane
[anesthesia] |
for induction and maintenance
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Remifentanyl
[anesthesia] |
an analgesia (small pain relief)
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Cisatracurium
[anesthesia] |
for relxation
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Etomidate
[IV anesthestic] |
rapid onset and moderately fast recovery
- CV stability, decreased steroidogenesis, invol muscle movements |
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*Raloxifene
(Evista) [Tx osteoporosis] |
Estrogen agonist on bone and antagonist in both breast and uterus.
- Reduce incidence of vertebral fractures - Best for prevention or tx of mild osteoporosis, spinal osteoporosis. - SE: hot flashes, leg cramps, blood clots. Does not increase risk of breast and uterine cancer and may reduce incidence of breast cancer |
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Alendronate (Fosamax)
***Ibandeonate (Boniva) Risedronate (***dronate) [osteoporosis tx] |
Biphosphonates
- inhibit osteoclastic activity and decrease bone turnover and resorption - reduce incidence of fractures in pts with osteo. - not well absorbed from GI tract and absorption is decreased more by presence of food. (low bioavailability, take with water only) - portion of absorbed drug is bound to bone (strong affinity for calcium phosphate); concentration in bone - osteoclasts that ingest these drugs more likely to undergo apoptosis = less resorption = fewer osteoclasts = more bone ex) Alendronate (Fosamax), Ibandeonate (Boniva), and Risedronate |
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Methylphenidate
(Ritalin) [ADD tx] |
RAS Stimulant - more commonly used
- short acting; onset 30 min, peak 1-3 hours single pulse or sustained release osmotic release (12 hr duration) or transdermal (more SE) - blocks the re-uptake of dopamine into presynaptic neurons, therefore increasing concentration of dopamine in RAS - SE: delayed sleep, headache, decreased appetite and weight loss |
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Amphetamine
(Adderall) [ADD tx] |
RAS stimulant
- short and long acting forms - blocks the re-uptake of dopamine into presynaptic neurons, therefore increasing concentration of dopamine in RAS - also increases release of Epi and NE - SE: delayed sleep, headache, decreased appetite and weight loss |
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Benzodiazepines
[for Anxiety] |
GABA agonists; Anxiolytic; opens chloride channels
- short term treatment for anxiety - enhances the affinity of GABA for its receptor - facilitating the opening of chloride channels through hyperpolarization; chloride flux -SE: sedation*, cognitive memory impairment ***** (alcohol potentiates sedative effects) - dependence and withdrawal symptoms can occur |
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Buspirone
(Buspar) [for Anxiety] |
Serotonin partial agonist; Anxiolytic
- for generalized anxiety disorder - full agonist at presynaptic 5HT receptors in raphe nuclei, AND as a partial agonist for postsynaptic 5HT receptors. (also has some D2 activity) = decreased firing of 5HT neurons and reduced release of 5HT NO activity at GABA receptor - SE: restlessness, nervousness (NOT sedating*) - partially effective when there are depressive sx or high levels of worry. Not as effective on autonomic sx such as increased HR - does not have effect of single dose and takes weeks for full therapeutic action |
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Zolpidem (Ambien)
Zaleplon (Sonata) Eszopiclone (Lunesta) [for anxiety] |
Non-benzo benzodoazepine receptor agonists; open chloride channels
- agonists at the GABA receptor but structurally not BZD; tricyclic absent - SE: drowsiness and lethargy (but still less sedating and less addictive than BZD) - limited dependene - can also be used or short-term treatment of insomnia |
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Carbamazepine
(Tegretol) [anti-epileptic] |
For generalized tonic-clonic, simple and complex partial, and partial with secondary generalization
- decrease repetitive firing; decreases Na current - liver metabolism, 80% protein bound - SE: drowsiness, transient diplopia, ataxia; hematological toxicity rare, agranulocytosis and aplastic anemia rare - fatal hepatitis has been reported *Autoinduction of its metabolism (normally have to give high doses to pts and liver gets overwhelmed so it increases enzymes to metabolize it, and drug will not be effective after some time |
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Phenytoin
(Dilantin) [anti-epileptic] |
seondary drug for generalized tonic-clonic, simple, complex partial
- blocks seizure spread, frequency dependent bloackade of Na channels - absorption slow, primarily liver metabolism - SE: Nystagmus common with therapeutic conc, drowsiness, ataxia, diplopia at high conc - gingival hyperplasia, coarse facial features and hirsutism can occur *autoinduce liver P450 enzymes so careful monitoruing |
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Valproic Acid
(Depakene) [anti-epileptic] |
primary for generalized tonic-clonic, may be used for petit mal
- increase GABA - hepatic metabolism - SE: serious SE uncommon, fatal liver failure has occured in children; may see wt gain, hair loss, rash, tremor, HA, insomnia, leukopenia, RBC aplasia, thrombocytopenia |
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Ethosuximide
(Zarontin) [anti-epileptic] |
********CHOICE drug for absence petit-mal seizures
- blocks calcium currents in thalamic neurons - liver metabolized; long half life but multiple dosing to minimize GI SE - SE: stomach aches, N/V, lethargy, hiccups and HA; skin rashes are most common |
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Metaclopramide
(Reglan) [migraine tx] |
D2 antagonist that stimulates release of ACh in myenteric plexus. increase gastric tone and accelerate gastric emptying
- has central effect - suppression of vomiting center |
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Domperidone
[migraine tx] |
D2 antogonist that stimulates release of ACh in myenteric plexus. increase gastric tone and accelerate gastric emptying
- does not cross BBB and has fewer CNS SE |
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*Cyclophosphamide
[cancer drug] |
a nitrogen mustard/alkylating agent
- most useful and versatile - activated by cytochrome P450 and interacts with DNA to inhibit synthesis - eliminated by kidney - USED for: *lymphoma, breast cancer, ovarian cancer, and oat cell lung cancer - SE: Myelosuppression; alopecia, immunosuppression and cystitis |
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*Methotrexate (MTX)
[cancer drug] |
Large folate antagonist/ antimetabolite
- competitively inhibits folic acid binding to dihydrofolate reductase and cell death occurs due to low levels of *thymidine [S-phase specific] - excreted by kidney - USED for: *ALL, Burkitt's lymphoma - SE: Myelosuppression - CI: do not use on patients with renal impairment - Interacts with salicylates and sulfonamides |
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Thioguanine
[cancer drug] |
Thiolated purine analog
- following type 1 lethal synthesis, it inhibits purine biosynthesis (1st step) and gets incorporated into DNA - excreted by kidney - USED for: Leukemias - SE: myelosuppression |
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5-fluorouracil (5-FU)
[cancer drug] |
Halogenated Pyrimidine Analog
- following Type 2 Lethal synthesis, it inhibits DNA synthesis by inhibiting *thymidylate synthetase --> TTP levels drop and gets incorporated into RNA - enters CNS and metabolized by liver - USED for: *Colon cancer, as well as breast, stomach, rectum, pancreas, liver and ovary - SE: Myelosuppression (often delayed) |
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Doxorubicin
[cancer drug] |
Anthracycline/anti-cancer antibody
- intercalating agents insert between DNA base pairs and bind tightly (intercalation) - [S-phase specific] - metabolized in liver - USED for: treating *solid tumors (breast, ovary, endometrium, bladder, thyroid, oat cell) - SE: Myelosuppressive and *Cardiac Toxic |
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Bleomycins
[cancer drug] |
Anti-cancer Antibody
- stand scission ; binds to DNA and cuts phosphate backbone - excreted in kidney - USED for: *testicular cancer, Hodgkin's and non-Hodgkin's lymphoma - SE: *lung toxicity and skin toxicity |
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Cisplatin
[cancer drug] |
Platinum Coordination Complex
- metal that forms strong complexes with DNA - excretion in kidneys - USED for: testicular cancer - SE: renal toxicity |
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*Vincristine
[cancer drug] |
Vinca Alkaloid Agent/plant derived product
- binds to tubulin and blocks polymerization to MT [M-phase specific] and leads to apoptosis - excreted in bile - USED for: ALL and Hodgkin's, non-Hodgkin's lymphoma - SE: neurological toxicity |
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Paclitaxel (Taxol)
[cancer drug] |
Taxane agent/plant derived agent
- binds to beta-tubulin and tubulin dimers and prevents MT disassembly = arrested in metaphase - cytochrome P450 - excreted in bile - USED for: Metastatic ovarian and breast cancers - SE: *myelosupressive, myalgias and *peripheral neuropathy |
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Prednisone
[cancer drug] |
- anti-inflammatory
- binds to hormone responsive elements (HRE) and alters transcription - Prednisone has the ability to destroy or limit lymphocytes so leukemias that result from uncontrolled growth of lymphocytes can be tx with prednisone - USED to induce remission in patients with ALL; as well as treat both Hodgkin and non-Hodgkin lymphomas - SE: immunosuppression, GI ulcers and pancreatitis |
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*Tamoxifen
[cancer drug] |
Sex Hormone Antagonist/Selective Estrogen Receptor Modulator (SERM)
- Estrogen antagonist that interferes wit action of estrogen in breast cancers - USED for: FIRST LINE therapy to treat Estrogen Receptor Positive Breast Cancer (+ phophylactic) (weak estrogenic activity) - SE: menopause like sx: hotflashes, nausea, fluid retention - 2x increase risk in endometrial cancer and *thromboembolic risk |
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Abarelix
[cancer drug] |
GnRH antagonist
- peptide antagonist of GnRH receptor - does not exhibit the flare phenomenon so therapeutically better - USED for: Prostate Cancer - SE: hot flashes, nausea, decreased bone |
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Anastrozole
[cancer drug] |
Aromatase inhbitor/Imidazole
- selective inhibition of aromatase results in less conversion of androgen to estrogen = decrease in estrogen - non-steroidal, more potent and selective - does not predispose to endometrial cancer and is devoid of androgenic side effects - USED for: advanced estrogen receptor positive and progesterone positive breast cancer - SE: *thromboembolism, fractures, cataracts |
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*Imatinib (Gleevec)
[cancer drug] |
Tyrosine Kinase inhibitor
- inhibitor of specific protein tyrosine kinases that was targeted to platelet-derived GF receptor - inhibits the fusion product from Philadelphia chromosome of Chronic Myelogenous Leukemia (CML) and c-kit which is overexpressed in GI stromal tumors (inhibits ATP binding to CML enzyme therefore no phosphorylation etc) - USED for: treatment of CML but also good for GI tumors - SE: retention, HA, NVD, swelling, rash, fever - Serious SE: reduced WBC, RBC, platelets, infection, internal bleeding, HF |
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*Bevacizumab
[cancer drug] |
Angiogenesis Inhibitor
- USED for: colorectal cancer that has spread, and some non-small cell lung cancers - SE; flu-like symptoms |
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***Allopurinol
[chronic gout drug] |
inhibitor of Xanthine Oxidase therefore lowering uric acid levels in blood
- preferable in patients with renal problems can be combined with probenecid or sulfinpyrazone |
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***Colchicine
[acute gout drug] |
Plant alkaloid that binds to microtubules leading to depolymerization
- reduced mobility of neutrophils, less lactic acid and fewer urate crystals - SE: nausea rarely causes myopathy or agranulocytosis |
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Gold Salts
[RA drug] |
for Rheumatoid Arthritis
- for those who do not respond to NSAIDs - inhibits maturation and function of mononuclear phagocytes and of T cells. concentrations in organs that are rich in phagocytes - selectively accumulates in lysosomes of type A synovial cells and MCP within inflamed synovium - SE: high toxicity, lesions in skin and mucosa membranes |
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Sulfonylurea
[anti-diabetic] |
stimulate insulin secretion from pancreatic beta cells
inhibit ATP sensitive K channels allowing influx of calcium and exocytosis of insulin - these do not decrease insulin resistance; does not affect insulin sensitivity *** must have functional pancreas - SE: Hypoglycemia so pt must eat after taking drug if given with thiazide diuretic, must increase sulfonylureas dose ACE, Warfarin, alcohol increase hypoglycemic effects of sulfonyurea renal disease decreases elimination of sulfonyurea and their metabolites - 2nd generations are used more ex) Glyburide, Amaryl |
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Metformin
(a Biguanide) [anti-diabetic] |
#1 PRESCRIBED!!!! IMPORTANT; for type II
decreases hepatic gluconeogenesis, decreases glucose absorption in the gut and increases insulin sensitivity in skeletal muscle and adipose tissue - requires presence of insulin which also decreases gluconeogenesis - does not stimulate insulin secretion ** does not cause hypoglycemia - may cause diarrhea, lactic acidosis |
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Acarbose
( a alpha-glucosidase inhibitor/starch blockers) [anti-diabetic] |
for Type 2 diabetes
inhibits alpha glucosidase - an enzyme in the intestinal brush border and will decrease CHO digestion and decrease disaccharide absorption - used to prevent post-prandial absorption in GI tract - SE: flatulence, abdominal cramping, diarrhea |
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Rosiglitazone and Pioglitazone
-litazone (TZDs) [anti-diabetic] |
Peroxisome proliferator-activaated receptor agonists
- Rosidlitazone has CV converns - Pioglitazone is contraindicated in bladder cancer - increases insulin sensitivity, glucose metabolism, atherosclerosis, adipocyte differentiation |
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Statins/Lovastatin
(cholesterol lowering) |
decreases blood lipid levels by inhibiting cholesterol synthesis
completely inhibits HMG-CoA reductase |
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Orlistat
(Alli) [lipid lowering] |
for obestiy; prevent absorption of fats in gut and reducing caloric intake by inhibiting gastric and pancreatic lipase
- SE: steatorrhea |
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Fibrates
[lipid lowering] |
activate lipoprotein lipase to decrease plasma lipid levels
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Ezetimibe
Niacin Probucol [treat hyperlipidemia] |
- all for treating hyperlipidemia
Ezetimibe prevents cholesterol absorption in intestine Niacin inhibits hormone-sensitive lipase Probucol prevents oxidation of LDL |
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Garlic
(Allicin) [herbal] |
Used for prevention of *common cold and heart disease
Lowers cholesterol, TGs, and BP Can be cancer preventative and antispetic - SE: odorous skin, bruising, *risk of bleeding, GI upset with HIV meds - DO NOT combine with anticoagulants or natural anticoagulants such as ginger or high dose Vit E |
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Ephedra
[herbal] |
first dietary supplement; also known as Ma Huang
- Used for *weight loss, used to stay awake - Effects: vasoconstriction, increased HR, CNS stimulation, increased plasma glucose, bronchodilation, decreases gastric emptying - SE: extreme *HTN, cardiomyopathy, dysrhythmias, MI, *stroke, seizure; hard to distinguish from schizophrenia - mixed with caffeine or other stimulants to stay awake (blue ecstasy, 7th heaven) |
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Ginko
[herbal] |
Improves cerebral circulation, *memory, alertness (alzheimer's pts use)
improves dementia, intermittent claudication, alleviates vertigo and tinnitus - SE: GI discomfort, seizures, may alter insulin in diabetes, *cerebral hemorrhage - do not combine with anticoagulants or naturals such as garlic and vitamin E - can cause HTN with thiazide diuretics |
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Ginseng
[herbal] |
increases stamina and concentration, *tonic invigoration
antioxidant, antineoplastic, improves blood sugar control - SE: tachycardia, *bleeding - Contraindicated with HTN and breast cancer, increases lab values with Digoxin |
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Echinacea
[Herbal] |
increases cytokine activity and *stimulates cellular immunity
- for minor respiratory infections, antiseptic/antiviral, *colds/flu, anti-inflammatory, antibacterial, peripheral vasodilator - SE: *allergic rxns, immune stimulating (HIV or autoimmune), transplants, erythema nodosum |
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St. John's Wort
[herbal] |
inhibits the uptake of dopamine, serotonin, and NE
inhibits monoamine oxidase in vitro potent inhibitor of P450 - Used for mild to moderate depression - SE: photosensitivity, N, fatigue, rash, prolonged PR interval, prolongs effects of narcotics - do not mix with antidepressants, melatonin - decreases the bioavailability of digoxin, cyclosporine |
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Saw Palmetto
[herbal] |
benefit for treatment of BPH
- antiandrogenic effect, anti-inflammatory |
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Radioactive Iodine
[tx hyperthyroidism] |
only isotope used to treat thyrotoxicosis by emitting beta rays toxic to cells
- an oral solution is rapidly absorpbed, concentrate by the thyroid and incorporated into storage follicles - the thyroid parenchyma is destroyed within few weeks, goal is to administer enough to result in euthyroid state without precepitating hypothyroidsim - only used in adults > 35 yo, not during pregnancy or nursing mothers |
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Propylthiouracil (PTU)*
(a Thiomide) [tx hyperthyroidism] |
compete for oxidized iodide causes decrease in thyroid hormone production
- inhibit thyroid-peroxidase catalyzed reactions, blocking iodine organification (conjugation) and inhibiting synthesis of thyroid hormones - *Also inhibits peripheral conversion of T4 to T3 - takes 6-8 weeks, do not inhibit release of stored thyroid hormones - SE: maculopapular pruitic rash with fever, severe agranulocytosis, arthralgias, decrease prothrombin and increased bleeding - crosses placenta but preferred during pregnancy bc more protein bound and crosses less readily -not secreted in breast milk |
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Methiamazole
[tx hyperthyroidism] |
compete for oxidized iodide causes decrease in thyroid hormone production
- inhibit thyroid-peroxidase catalyzed reactions, blocking iodine organification (conjugation) and *inhibiting synthesis of thyroid hormones - does not inhibit T4 to T3 conversion - SE: maculopapular pruitic rash with fever, severe agranulocytosis, arthralgias - crosses placenta -not secreted in breast milk |
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Levothyroxine [T4]
[tx hypothyroidism] |
thyroid replacement must be weighed against risk of precipitating MI
- T4 for GI absorption, entirely bound to plasma proteins |
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Triiodothyronine [T3]
[tx hypothyroidism] |
increased metabolic activity and short half-life makes this less satisfactory for therapy
- only standardized for iodine content and should not be used |
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Somatropin
[hypothalamic and pituitary drugs] |
GH is enhanced by GHRH and inhibited by somatostatin; fail to secrete GH during puberty results in growth retardation most frequently d/t defective hypothalamic release of GHRH
- Somatotropin is a recombinant human growth hormone used for GH replacement therapy |
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Carbegoline
[hypothalamic and pituitary drugs] |
Lactotrophs of AP secrete prolactin which suppresses estrogen synthesis by antagonizing hypothalmic release of GnRH and decreases sensitivity to GnRH
- Cabergoline is a dopamine receptor agonist that can decrease prolactin levels - used for medical therapy for small prolactinomas - SE: N/V |
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Leuprolide
[hypothalamic and pituitary drugs] |
A GnRH agonist that is injected once daily
- act as partial agonist in stimulating the secretion of LH and FSH, causing a resulting transient increase in testosterone levels. Subsequently there is a decrease in testosterone d/t a desensitization of GnRH receptors in pituitary - can be given to men to aid in mgmt of early stage Prostate Cancer which is androgen dependent |
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Follitropin
[hypothalamic and pituitary drugs] |
Hormone Replacement Therapy for in vitro fertilization
- recombinant form of FSH - stimulates ovulation but may cause ovarian hyperstimulation syndrome |
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Desmopressin
[Posterior pituitary drug] |
ADH stimulates water reabsorption in CD and increases BP
- Desmopressin is an ADH analog and can be used to **treat Neurogenic Diabetes Insipidus (hypothalamic neurons are unable to synthesize ADH |
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Oxytocin
[Posterior pituitary drug] |
peptide hormone known to mediate muscle contraction (milk release during lactation and uterine contraction)
- used to induce labor artificially |
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Some old drugs
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Enfuviritide: HIV fusion inhibitor
Oseltamivir (Tamiflu): treat certain influenza who have had sx no longer than 3 days Rifampin: antibiotic, Anti-TB - inhibits RNA poly ddl; AZT: antiviral, inhibit DNA synthesis FQ/cipro: antibiotic, inhibit DNA gyrase Metronidazole/flagyl: antibtioc to treat bacterial and parasitic infections Tetracycline: antibiotic; inhibit bacterial protein synthesis Prednisone: anti-inflammatory, inhibits PL --> less PG and LT Cyclosporine, Rapamycin: inhibit helper T cell activation to prevent rejection of transplant Heparin: activates anti-thrombin for anti-coagulation Warfarin/Coumadin: Vit K antagonist as anti-coagulant Hydrochlorothiazide: diuretic, inhibits retention and decreases blood volume (SE of hypokal/mag/nat) |
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More more old drugs
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Disulfiram - inhibits aldehyde dehydrogenase = treat alcoholics
Bethanechol, Carbachol, Methacoline = cholinergic agonist for Autonomic nervous system Pilocarpine = muscarine agonist; treats dry mouth Edrophonium, neostigmine, pyridostigmine: ACh esterase inhibitors to treat myasthesia gravis Atropine: muscarinic blocker, tx organophosphate poisoning Pralidoxime: antidote to nerve gas poisoning; recovers ACh esterase Sarin/organophosphates: irreversible inhibotir of ACh inhibitors - nerve gas Echothiaphate - irreverisble inhibitor of ACh inhibitors - used to treat glaucoma Terazosin (**azosin): alpha 1 blocker to treat HTN Tamsulosin (flomax): alpha 1 blocker, used to treat BPH Aldomet: choice anti HTN during pregnancy; alpha 2 agonist Clonidine: alpha 2 agonist, ER anti-HTN Dobutamine: beta 1 agonist - for tx of HF, pumps blood |
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even more old drugs + diuretics)
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-butolol: b1 blockers to slow down HR
-terol, Terbutaline: beta 2 agonist to tx asthma and COPD Ritodrine: beta 2 agonist to treat premature uterine contractions Diphenhydramine (Benadryl): H1 blocker to treat allergies Nifedipine (-dipine) and Verapamilare CCB, anti HTN Spironolactone: K sparring diuretic: ALDP antagonist Furosemide (Lasix): loop diuretic to treat HTN Chlorothiazide: thiazide diuretic for HTN -pril: ACEI to treat HTN Losartan (sartan): angiotensin receptor blocker - treat hypertension - Propofol (diprivan): general anesthesia, decrease GABA |
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Dantrolene
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Treatment for Malignant Hyperthermia
Treatment for Neuroleptic Malignant Syndrome |
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Celecoxib
(Celebrex) |
Sulfonamide NSAID, COX 2 inhibitor only; treats pain
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