pharm test 2 2
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- LDL: Friedwald equation
- LDL = TC - [HDL +(TG/5)].....not valid if TG > 400
- 2ary hyperlipidemia: endocrine causes
- diabetes mellitus, hypothyroidism
- 2ary hyperlipidemia: drug induced
- HIV protease inhibitors
- 2ary hyperlipidemia: renal
- nephrotic syndrome
- 2ary hyperlipidemia: hepatic
- cholestatic liver disease
- cholestyramine: class
- bile acid sequestrant
- cholestyramine: mechanism
- bind bile acids
- cholestyramine: dosing
- given with meals
- cholestyramine: side effects
- GI, absorption of other drugs
- cholestyramine: indications
- kids; moderate LDL 2nd line; combo therapy for bad LDL
- cholestyramine: interactions
- bind other drugs
- cholestyramine: effect on total cholesterol
- decrese
- cholestyramine: effect on LDL
- decrease
- cholestyramine: effect on HDL
- increase
- cholestyramine: effect on serum triglycerides
- no effect
- colestipol: class
- bile acid sequestrant
- colestipol: mechanism
- bind bile acids
- colestipol: dosing
- given with meals
- colestipol: side effects
- GI, absorption of other drugs
- colestipol: indications
- kids; moderate LDL 2nd line; combo therapy for bad LDL
- colestipol: interactions
- bind other drugs
- colestipol: effect on LDL
- decrease
- colestipol: effect on HDL
- increase
- colestipol: effect on serum triglycerides
- no effect
- bile acid sequestrants: mechanism
- bind bile acids
- bile acid sequestrants: 1st line which pts
- children
- bile acid sequestrants: dosing
- given with meals
- bile acid sequestrants: side effects
- GI, absorption of other drugs
- bile acid sequestrants: indications
- kids; moderate LDL 2nd line; combo therapy for bad LDL
- bile acid sequestrants: interactions
- bind other drugs
- bile acid sequestrants: effect on LDL
- decrease
- bile acid sequestrants: effect on HDL
- increase
- bile acid sequestrants: effect on serum triglycerides
- no effect
- ezetimibe: class
- cholesterol absorption inhibitors
- ezetimibe: mechanism
- inhibit cholesterol absorption at brush border of small intestine
- ezetimibe: indications
- adjunct to statins
- ezetimibe: pharmacokinetics
- prodrug absorbed and converted to active glucuronide and excreted into gut where it is active
- ezetimibe: interactions
- bound by bile acid resins
- ezetimibe: effect on LDL
- decrease (biggest effect)
- ezetimibe: effect on HDL
- no effect
- ezetimibe: effect on serum triglycerides
- decrease
- ezetimibe: predominiant serum lipid effect
- decrease LDL
- cholesterol absorption inhibitors: mechanism
- inhibit cholesterol absorption at brush border of small intestine
- cholesterol absorption inhibitors: indications
- adjunct to statins
- cholesterol absorption inhibitors: interactions
- bound by bile acid resins
- cholesterol absorption inhibitors: effect on LDL
- decrease (biggest effect)
- cholesterol absorption inhibitors: effect on HDL
- no effect
- cholesterol absorption inhibitors: effect on serum triglycerides
- decrease
- cholesterol absorption inhibitors: predominiant serum lipid effect
- decrease LDL
- gemfibrozil: class
- fibric acid derivative
- gemfibrozil: mechanism
- PPAR receptor agonist, induce TG metabolism and clearance
- gemfibrozil: indications
- high triglyceride hyperlipidemia
- gemfibrozil: interactions
- statins and gemfibrozil--risk of skeletal muscle dysfunx
- gemfibrozil: effect on total cholesterol
- decrease
- gemfibrozil: effect on LDL
- decrease (usually)
- gemfibrozil: effect on HDL
- increase
- gemfibrozil: effect on serum triglycerides
- decrease
- gemfibrozil: predominiant serum lipid effect
- reduce triglyceride containing lipoproteins
- fibric acid derivatives: mechanism
- PPAR receptor agonist, induce TG metabolism and clearance
- fibric acid derivatives: indications
- high triglyceride hyperlipidemia
- fibric acid derivatives: effect on total cholesterol
- decrease
- fibric acid derivatives: effect on LDL
- decrease (usually)
- fibric acid derivatives: effect on HDL
- increase
- fibric acid derivatives: effect on serum triglycerides
- decrease
- fibric acid derivatives: predominiant serum lipid effect
- reduce triglyceride containing lipoproteins
- Statins: mechanism
- competitive inhibition of HMG CoA reductase; upregulation of LDL receptors; decreased de novo cholesterol and VLDL
- Statins: 1st line which pts
- hypercholesterolemia w/ increased LDL
- Statins: excretion
- metabolized by liver and excreted in bile
- Statins: metabolism
- metabolized in liver, big 1st pass effect
- Statins: adverse effx
- skeletal muscle dysfnx--risk increased with gemfibrozil or CYP 3A inhibitors
- lovastatin: class
- statin
- lovastatin: mechanism
- competitive inhibition of HMG CoA reductase; upregulation of LDL receptors; decreased de novo cholesterol and VLDL
- lovastatin: dosing
- given with food to enhance absorption
- lovastatin: excretion
- metabolized by liver and excreted in bile
- lovastatin: metabolism
- metabolized in liver, big 1st pass effect
- HMG CoA reductase: fnx
- regulatory enzyme in cholesterol biosynthesis
- Niacin: chemistry
- nicotinic acid
- Niacin: mechanism
- complex: affects synthesis and metabolism of cholesterol and triglycerides
- Niacin: adverse effx
- flushing from PGD2 release (aspirin alleviates)
- niaspan: class
- controlled release niacin
- niaspan: 1st line which pts
- familial hyperlipidemia w/ inc VLDL and LDL, and in hyperlipoprotenemias with elevated VLDL
- Strychnine : class
- analeptic/conglusant
- Strychnine : mechanism
- inhibits GABA in CNS
- Strychnine : adverse effx
- tonic extensino of body and limbs
- Strychnine : tx of poisoning
- diazepam
- picrotoxin: class
- analeptic/conglusant
- picrotoxin: mechanism
- inhibits Glycine in spine
- picrotoxin: adverse effx
- generalized tonic clonic
- picrotoxin: tx of poisoning
- diazepam
- caffeine: class
- methylxanthines stimulatant
- caffeine: mechanism
- action at adenosine receptors (A1 and A2)
- theophylline: class
- methylxanthines stimulatant
- theophylline: mechanism
- action at adenosine receptors (A1 and A2)
- theobromine: class
- methylxanthines stimulatant
- theobromine: mechanism
- action at adenosine receptors (A1 and A2)
- amphetamine: mechanism
- promotes release of NE and DA; inhibits reuptake
- amphetamine: indications
- narcolepsy, ADD, weight loss
- amphetamine: route
- oral
- amphetamine: time to peak plasma conc
- 1 to 3 hours
- amphetamine: urine pH and clearance
- high pH, metabolic; low pH, urine
- cocaine: mechanism
- blocks reuptake of NE, DA, and 5HT
- cocaine: half life
- ~ half hour
- cocaine: Spanish
- la cocaína
- cocaine: French
- la cocaïne
- cocaine: Arabic
- الكوكائين
- cocaine: Chinese
- å¯å¡å› (kÄ›kÇŽyÄ«n)
- nonamphetimine: narcolepsy
- modafinil
- nonamphetimine: ADD
- methylphenidate
- nonamphetimine: weight loss
- fenfluaramine, phentermine
- ergot compounds (LSD): class
- indolalkylamine, chemically related to 5HT
- indolamines: class
- indolalkylamine, chemically related to 5HT
- beta carboines: class
- indolalkylamine, chemically related to 5HT
- mescaline: class
- phenylethylamine, chemically related to dopamine
- amphetamine derivatives: class
- phenylethylamine, chemically related to dopamine
- LSD: half life
- 3 hours
- psylocybin: class
- indolalkylamine resembling serotonin. Tryptamine derivative
- hallucinagens: mechanism
- agonists of 5HT(2A) subtype
- hallucinagens: tolerance
- yup
- hallucinagens: physical dependence
- nope
- Phencyclidine : mechanism
- blocks NMDA receptors (subset of glutamate receptors)
- benzodiazepine: mechanism
- enhance GABA-ergic transmission, self limiting effect
- benzodiazepine: side effects
- decreased alertness, ataxia (problem for elderly, hp fx)
- benzodiazepine: tolerance
- yeah
- benzodiazepine: physical dependence
- yeah
- benzodiazepine: effect on dose resonse curve of GABA
- increased potency, unaffected efficacy
- benzodiazepine: antidote
- Flumazenil
- diazepam: class
- benzodiazepine
- diazepam: trade name
- valium
- chordiazepoxide: class
- benzodiazepine
- chordiazepoxide: trade name
- librium
- lorazepam: class
- benzodiazepine
- lorazepam: excretion
- glucoronidation
- lorazepam: trade name
- ativan
- lorazepam: duration
- short
- midazolam: class
- benzodiazepine
- midazolam: excretion
- hydroxylation and glucoronidation
- midazolam: trade name
- versed
- midazolam: duration
-
short
(diazapine) - buspirone: mechanism
- erotonergic agonists acting at the 5HT1A
- buspirone: clinical effect
- anti anxiety
- Zolpidem : clinical effect
- sleep aid
- ethanol: cytochrome intx
- augments metabolism of CYP 450
- methanol: antidote
- 4-methylpyrazole, and ethanol
- methanol: toxicity
- anion gap acidosis, blindness
- ethelyne glycol: toxicity
- oxalate crystals in urine, anion gap acidosis
- delirium tremens: tx
- diazepine, (watch out diazepam if liver disease)
- Chlorpromazine : class
- phenothiazine and related antipsychotic
- reserpine: class
- rauwolfia alkaloids antipsycotic
- reserpine: mechanism
- blockade of D2 receptors
- neuroleptics: effect at reticular activating system
- depression
- neuroleptics: effect at mesolimbic dopamine system
- reduction in psychosis
- neuroleptics: effect at mesocortical system
- increased negative sx of schizo
- neuroleptics: effect at nigrostriatal system
- parkinsonian like sx
- neuroleptics: effect at hypothalamus
- poikilothermia, increase prolactin
- neuroleptics: time till effect
- 3-6 weeks
- neuroleptics: neuroleptic malignant syndrome characteristics
- muscular rigidity; fever; elevated CPK
- haloperidol: class
- depot antipsychotic
- risperidone microspheres: class
- depot antipsychotic
- depot antipsychotic: advantages
- compliance not problem
- depot antipsychotic: disadvantages
- increased risk of side effx
- neuroleptic malignant sydrome: tx
- datrolene, fever reduction, keep 'em alive
- typical antipsychotics: protein binding
- 0.9
- clozapine: class
- atypical antipsychotic
- clozapine: mechanism
- blockade of 5HT2a/2c, which stimulates dopamine release in mesolimbic area
- clozapine: side effects
- agranulocytosis
- Risperidone : class
- atypical antipsychotic
- Risperidone : mechanism
- Mixed D2 - 5HT2a effects (most prominent D2 of atypical class)
- Olanzapine : class
- mood stabalizer
- Olanzapine : mechanism
- Receptor binding affinity almost identical to clozapine (5HT2a, weak D2)
- Aripiprazole : class
- atypical antipsychotic
- Aripiprazole : mechanism
- D2 partial agonist
- phenelzine : class
- Hydrazines MAO inhibitor
- phenelzine : side effects
- hypotension, antisymp sx; tyramine induced hypertension
- tranylcypromine : class
- nonhydrazine MAO inhibitor
- tranylcypromine : side effects
- hypotension, antisymp sx; tyramine induced hypertension
- MAO inhibitor: side effects
- hypotension, antisymp sx; tyramine induced hypertension; fat, can't fuck
- MAO inhibitor: indications
- depresssion and anxiety disorders
- MAO inhibitor: interactions
- central serotonin syndrome, central symp sydrome, reduced metabolism some drugs
- MAO inhibitor: inhibit metabolism of what drugs
- pseudoephedrine, phenylpropanolamine; meperidine
- amitryptyline: class
- tricyclic
- amitryptyline: mechanism
- block monoamine reuptake
- amitryptyline: side effects
- cholinergic blockade; a1 receptor inhibition (orthostatic hypo); histamine blockade (drowsy, weight gain), extra symp (cant fuck
- amitryptyline: indications
- depresssion and anxiety disorders
- nefadazone: class
- heterocyclic
- nefadazone: mechanism
- block monoamine reuptake
- nefadazone: side effects
- cholinergic blockade; a1 receptor inhibition (orthostatic hypo); histamine blockade (drowsy, weight gain), extra symp (cant fuck
- nefadazone: indications
- depresssion and anxiety disorders
- nefadazone: cytochrome metabolism
- CYP P450 3A4 (cyclosporine)
- fluoxetine: class
- SSRI
- fluoxetine: mechanism
- block serotonin reuptake
- fluoxetine: side effects
- cholinergic blockade; a1 receptor inhibition (orthostatic hypo); histamine blockade (drowsy, weight gain), extra symp (cant fuck
- fluoxetine: indications
-
OCD, depression
(SSRI) - fluoxetine: cytochrome metabolism
- CYP P450, competitively inhibit (inc beta blockers)
- sertaline: class
- SSRI
- sertaline: mechanism
- block serotonin reuptake
- sertaline: side effects
- cholinergic blockade; a1 receptor inhibition (orthostatic hypo); histamine blockade (drowsy, weight gain), extra symp (cant fuck
- sertaline: indications
- depression, panic
- sertaline: cytochrome metabolism
- CYP P450, competitively inhibit (inc beta blockers)
- paroxetine: class
- SSRI
- paroxetine: mechanism
- block serotonin reuptake
- paroxetine: side effects
- cholinergic blockade; a1 receptor inhibition (orthostatic hypo); histamine blockade (drowsy, weight gain), extra symp (cant fuck
- paroxetine: indications
- OCD
- paroxetine: cytochrome metabolism
- CYP P450, competitively inhibit (inc beta blockers)
- tricyclic & related with dopamine blockade: side effects
- more psychosis
- tricyclics: heart side efx
- Ia antiarrhythmics, AV block
- SSRIs: cytochrome metabolism
- CYP P450, competitively inhibit (inc beta blockers)
- Lithium: class
- mood stabalizer
- Lithium: mechanism
- inhibit Gs proteins and antagonize phospholipase C (probably)
- Lithium: side effects
- hypothyroidism (weight gain); polydypsia, interstitial nephritis; heart conduction problems; birth defects
- Lithium: indications
- typical bipolar I
- Lithium: interactions
- diuretics decrease clearance; NSAIDS increase plasma level (not aspoirin); neuromuscular drugs potentiated
- Lithium: contraindx
- sick sinus synd; pregnancy
- Lithium: alternatives in biopolar (3 from lecture)
- Carbamazepine; divalproex; olanzapine
- carbamazepine: class
- mood stabalizer
- carbamazepine: mechanism
- inhibit Gs proteins and antagonize phospholipase C (probably)
- divalproex: chemistry
- valproic acid
- divalproex: class
- mood stabalizer
- divalproex: mechanism
- inhibit Gs proteins and antagonize phospholipase C (probably)
- divalproex: indications
- bipolar i and ii
- Olanzapine : intracellular mechanism
- inhibit Gs proteins and antagonize phospholipase C (probably)
- fast pain: fiber type
- A delta (myelinated)
- slow pain: fiber type
- C (unmyelinated)
- hyperalgesia/allodynia: involved nerurecepter type in dorsal horn neurons
- substance P receptor (NMDA(
- analgesia: involved nerurecepter type in dorsal horn neurons
- mu opiate receptor; alpha 2 adrenergic
- endomorphins: involved nerurecepter type in dorsal horn neurons
- mu opiate receptor
- morphine: class
- opiate
- morphine: mechanism
- binds mu opiate receptor
- morphine: side effects
- itcing (histamine release); puking
- morphine: involved nerurecepter type in dorsal horn neurons
- mu opiate receptor
- morphine: effect at D2 receptors
- agonist
- morphine: first pass effect
- stupid big
- morphine: bioavailability
- under 50%
- codeine: class
- opiate
- codeine: bioavailability
- 0.7
- meperidine: class
- opiate
- meperidine: side effects
- neurotoxicity; only short term
- meperidine: indications
- p
- meperidine: contraindx
- end stage renal failure
- fentanyl: class
- opiate
- methadone: class
- opiate
- naloxone: class
- opiate antagonist
- naloxone: indications
- opiate toxicity
- naloxone: duration
- under hour
- opiate overdose: signs
- miosis (small pupils); slow, shallow resp; coma
- opiate overdose: tx
- naloxone
- status epilepticus: best tx
- lorazepam followed by fosphenytoin