Flashcards in B2 Drug Names Deck (247):
1
Ibuprofen
Reversibly inhibits Cox 1 and 2
2
Succinylcholine
Depolarizing NM blocker
3
Baclofen
Spasmalytic: GABA B agonist
increased K flow-->hyper polarization--> reduces release of excitatory NT
4
Simvastatin
Hypolipidemic: Competitive HMG-CoA reductase inhibitor (rate-limiting step of cholesterol synthesis) and induces high affinity LDL receptors--> reduces LDL levels
Toxicity = myositis and sometimes rhabdomyolysis (monitor creatine kinase) and hepatotoxicity (monitor liver enzymes)
Drugs that inhibit CYP enzymes will increase plasma concentrations of statins!!!
5
Cholestyramine
Bile Acid Binding Resin: Binds BA in intestine and forms complex that's excreted in feces.
Increased oxidation of cholesterol to BA in liver and increased # of LDL receptors--> decreased LDL levels and increased HDL
Toxicity: constipation, deficiency of fat-soluble vitamins (A, D, E, K)
May also delay or reduce the absorption of other oral medications (digitalis, warfarin)
CONTRAINDICATED in patients with hypertriglyceridemia
6
Gemfibrozil
HYPOlipidemic:
agonist at PPAR alpha and INCREASES the activity of LPL (esp in muscles and hepatocytes) --> hyperTG and reduces VLDL
Toxicity:
- GI symptoms
- myopathy
- cholesterol gallstones
Drug interactions: can displace other albumin-bound drugs like warfarin and sulfonyl ureas
7
D- Tubocurarine
Competitive Nm blocker
8
Bile acid binding resins are contraindicated in whom?
patients with hypertriglyceridemia
9
Tizanidine
alpha 2 agonist used as a spasmolytic --> decreases m tone without causing paralysis
10
pravastatin
Hypolipidemic: Competitive HMG-CoA reductase inhibitor (rate-limiting step of cholesterol synthesis) and induces high affinity LDL receptors--> reduces LDL levels
Toxicity = myositis and sometimes rhabdomyolysis (monitor creatine kinase) and hepatotoxicity (monitor liver enzymes)
Drugs that inhibit CYP enzymes will increase plasma concentrations of statins!!!
11
colestipol
Bile Acid Binding Resin: Binds BA in intestine and forms complex that's excreted in feces.
Increased oxidation of cholesterol to BA in liver and increased # of LDL receptors--> decreased LDL levels and increased HDL
Toxicity: constipation, deficiency of fat-soluble vitamins (A, D, E, K)
May also delay or reduce the absorption of other oral medications (digitalis, warfarin)
CONTRAINDICATED in patients with hypertriglyceridemia
12
Vecuronium
Competitive Nm blocker
13
Niacin
hypolipidemic: inhibition of VLDL synthesis and esterification of FA in liver --> decreased plasma LDL, VLDL and TG levels!
Toxicity:
- flushing
- itching (treated by aspirin or other NSAID)
- diarrhea
- hyperuricemia (gout)
- hyperglycemia
14
Using what drugs along with statins causes an increased risk of myopathy?
- amiodarone
- verapamil
- fibrates
15
Dantrolene
Tx malignant hyperthermia
inhibits release of Ca from SR during excitation/contraction coupling
also inhibits ryanodine receptor and Calcium channels in skeletal m
16
lovastatin
Hypolipidemic: Competitive HMG-CoA reductase inhibitor (rate-limiting step of cholesterol synthesis) and induces high affinity LDL receptors
--> reduces LDL levels
Toxicity = myositis and sometimes rhabdomyolysis (monitor creatine kinase) and hepatotoxicity (monitor liver enzymes)
Drugs that inhibit CYP enzymes will increase plasma concentrations of statins!!!
17
pancuronium
Competitive Nm blocker
18
colesevelam
Bile Acid Binding Resin: Binds BA in intestine and forms complex that's excreted in feces.
Increased oxidation of cholesterol to BA in liver and increased # of LDL receptors--> decreased LDL levels and increased HDL
Toxicity: constipation, deficiency of fat-soluble vitamins (A, D, E, K)
May also delay or reduce the absorption of other oral medications (digitalis, warfarin)
CONTRAINDICATED in patients with hypertriglyceridemia
19
How do you treat parities (itching) caused by Niacin?
aspirin or other NSAID
20
Gabapentin
spasmolytic
21
Fenofibrate
HYPOlipidemic:
agonist at PPAR alpha and INCREASES the activity of LPL (esp in muscles and hepatocytes) --> hyperTG and reduces VLDL
Toxicity:
- GI symptoms
- myopathy
- cholesterol gallstones
Drug interactions: can displace other albumin-bound drugs like warfarin and sulfonyl ureas
22
doxacurium
Competitive Nm blocker
23
Ezetimibe
HYPOlipidemic
reduces GI absorption of cholesterol--> reduces LDL and TG
Toxicity: diarrhea, abdominal pain
24
Vigabatrin
Anti-epileptic drug
MOA: irreversibly inhibits GABA transaminase (GTA)
25
Epinephrine
Bronchodilator (lasts 60-90m); rapid action
also used in anaphylactic shock (is a physiological antagonist)
Given Subcutaneous/Inhalation
--> tachycardia, arrhythmias
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
26
Prednisolone
oral systemic corticosteroid
MOA: Has anti-inflammatory effects. Binds to an internuclear receptor and inhibits the transcription of genes that are responsible for producing cytokines. ESP interleukins
Use: severe chronic asthma
Chronic use can lead to Cushing's Disease
A/E:
- easy brushing
- adrenal suppression
- growth retardation
- increased bone catabolism--> osteoporosis
27
Rocuronium
Competitive Nm blocker
28
Tiotropium Bromide
Bronchodilator: given via inhalation; long acting (24h)
MOA: parasympathetic! Blockage of muscarinic receptors: anticholinergics
Blocks muscarinic receptors in large airways
frequently used in combo with salbutamol (DOC for people on beta blockers)
29
Tiagabine
Anti-epileptic drug
MOA: blocks GABA reuptake by blocking GAT (GABA transporter)
30
Isoproterenol
Bronchodilator
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
31
Ipratropium Bromide
Bronchodilator: given via inhalation; short acting, slower response
MOA: parasympathetic! Blockage of muscarinic receptors: anticholinergics
Blocks muscarinic receptors in large airways
frequently used in combo with salbutamol (DOC for people on beta blockers)
32
Levetriracetam
Anti-epileptic drug: treats GTC, simple partial seizures
MOA: binds to synaptic vesicular protein (SV2A) --> decreases synaptic release of glutamate
33
Hydrocortisone
IV systemic corticosteroid
MOA: Has anti-inflammatory effects. Binds to an internuclear receptor and inhibits the transcription of genes that are responsible for producing cytokines. ESP interleukins
Use: status asthmatics
Chronic use can lead to Cushing's Disease
A/E:
- easy brushing
- adrenal suppression
- growth retardation
- increased bone catabolism--> osteoporosis
34
DOC for asthmatics on beta-blockeres
Ipratropium Bromide in combo with Salbutamol
35
Albuterol
Bronchodilator: onset 5-15m
given via metered dose inhaler, nebulizer, oral tablet
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
How: stimulates AC --> increase cAMP
Use: acute attacks and maintenance
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
36
Theophylline
BRONCHODILATOR
MOA: inhibition of phosphodiesterase--> increase cAMP
Narrow therapeutic margin (5-20; A/E above 25)--MONITOR serum levels to avoid toxicity!
Eliminated via CYP450
Slow-release form used to treat nocturnal asthma
Add on Rx where inhaled steroid plus beta agonist ineffective!
A/E:
CNS stimulant: insomnia, tremor, convulstions
heart: positive chronotropic and inotropic effect
Weak vasodilator
weak diuretic
anxiety
tachycardia
diuresis
vomiting
arrhythmia
shock
37
Felbamate
Anti-epileptic drug
MOA: Blocks NMDA (glutamate) receptors
38
Beclomethasone
Inhaled Corticosteroid. Used to treat Asthma. High topical and low systemic activity
MOA: Has anti-inflammatory effects. Binds to an internuclear receptor and inhibits the transcription of genes that are responsible for producing cytokines. ESP interleukins
A/E:
- dysphonia
- oropharyngeal candidia (brush teeth after puffing inhaler for prevention)
- sore throat
39
Terbutaline
Bronchodilator
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
40
Zileuton
Leukotriene Synthesis Inhibitor: used in aspirin-induced asthma
MOA: Leukotriene Synthesis Inhibitor: 5-lipoxygenase inhibitor
A/E: Hepatotoxicity; elevation of liver enzymes must be monitored
41
Gabapentin
Anti-epileptic drug
MOA: Binds to presynaptic voltage-gated N type of Ca channel --> decreases synaptic release of glutamate
42
A/E associated with Theophylline
A/E:
CNS stimulant: insomnia, tremor, convulstions
heart: positive chronotropic and inotropic effect
Weak vasodilator
weak diuretic
anxiety
tachycardia
diuresis
vomiting
arrhythmia
shock
43
Formeterol
Bronchodilator
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
44
Budesonide
Inhaled Corticosteroid. Used to treat Asthma. High topical and low systemic activity
MOA: Has anti-inflammatory effects. Binds to an internuclear receptor and inhibits the transcription of genes that are responsible for producing cytokines. ESP interleukins
A/E:
- dysphonia
- oropharyngeal candidia (brush teeth after puffing inhaler for prevention)
- sore throat
45
Pregbalin
Anti-epileptic drug
MOA: Binds to presynaptic voltage-gated N type of Ca channel --> decreases synaptic release of glutamate
46
Chlorpromazine
Phenothiazine typical antipsychotic
MOA: D2 receptor antagonist
Schizophrenia: reduce + symptoms
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Tardive dyskinesias (occurs very late):
- oral/facial dyskinesias, muscle jerks, writhing lip muscles
- caused by relative cholinergic deficiency secondary to supersensitivty of DA receptors
- More common in pots taking typical antipsychotics
- Tx: switch patient to atypical drug (quetiapine or clozapine)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
Hyperprolactinemia: weight gain
47
Montelukast
leukotriene receptor antagonist: Used as prophylaxis and chronic asthma treatment
Blocks bronchoconstriction, reduces edema, and decreases mucous production
MOA: competitively blocks LTD4, LTE4 receptors
48
Salmeterol
Bronchodilator: onset = 20, long-acting (DOA = 12h);
given via inhalation
Used for prophylaxis (prevents bronchoconstriction at night). NOT used for tx of acute asthma bc delayed onset!
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
49
Lamotrigine
Anti-epileptic drug: treats GTC, simple partial seizures
MOA: prolongs inactivation of Na channels, presynaptic voltage gated N type of Ca channel --> decreases synaptic release of glutamate
50
Fluticasone
Inhaled Corticosteroid. Used to treat Asthma. High topical and low systemic activity
MOA: Has anti-inflammatory effects. Binds to an internuclear receptor and inhibits the transcription of genes that are responsible for producing cytokines. ESP interleukins
A/E:
- dysphonia
- oropharyngeal candidia (brush teeth after puffing inhaler for prevention)
- sore throat
51
Extrapyramidal syndrome and treatment
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
52
Neuroleptic Malignant Syndrome and treatment
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
53
Zonisamide
Anti-epileptic drug: tx myoclonic seizures
MOA: block high frequency firing via action on Na channels
54
Zafirlukast
leukotriene receptor antagonist: Used as prophylaxis and chronic asthma treatment
Blocks bronchoconstriction, reduces edema, and decreases mucous production
MOA: competitively blocks LTD4, LTE4 receptors
55
Triamcinolone
Inhaled Corticosteroid. Used to treat Asthma. High topical and low systemic activity
MOA: Has anti-inflammatory effects. Binds to an internuclear receptor and inhibits the transcription of genes that are responsible for producing cytokines. ESP interleukins
A/E:
- dysphonia
- oropharyngeal candidia (brush teeth after puffing inhaler for prevention)
- sore throat
56
Benztropine
anti-muscarinic drug used to treat Extrapyramidal syndrome:
due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
57
Tardive dyskinesias and treatment
Tardive dyskinesias (occurs very late):
- oral/facial dyskinesias, muscle jerks, writhing lip muscles
- caused by relative cholinergic deficiency secondary to supersensitivty of DA receptors
- More common in pots taking typical antipsychotics
- Tx: switch patient to atypical drug (quetiapine or clozapine)
58
Typical Anti-psychotics:
end in "-zine" and haloperidol
59
Haloperidol
Typical Anti-psychotic;
used to treat touter's syndrome and to reduce + symptoms in Schizophrenia
MOA: D2 receptor antagonist
60
Sodium Cromoglycate
Inhaled mast cell stabilizer used in prophylaxis of asthma, allergic rhinitis, allergic conjunctivitis
MOA: inhibits degranulation of mast cell by trigger stimuli
61
Biperiden
anti-muscarinic drug used to treat Extrapyramidal syndrome:
due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
62
Sumatriptan
5HT1 receptor agonist
MOA: 5HT1D agonist
Use: acute migraine attack
63
Bromocriptine
Ergot Alkaloid that acts in the CNS
used to treat hyperprolactinemia and parkinson's disease
64
Fluphenazine
Phenothiazine typical antipsychotic
MOA: D2 receptor antagonist
Schizophrenia: reduce + symptoms
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Tardive dyskinesias (occurs very late):
- oral/facial dyskinesias, muscle jerks, writhing lip muscles
- caused by relative cholinergic deficiency secondary to supersensitivty of DA receptors
- More common in pots taking typical antipsychotics
- Tx: switch patient to atypical drug (quetiapine or clozapine)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
Hyperprolactinemia: weight gain
65
Nedocromil
mast cell stabilizer used in prophylaxis of asthma, allergic rhinitis, allergic conjunctivitis
MOA: inhibits degranulation of mast cell by trigger stimuli
66
trihexphenyl
anti-muscarinic drug used to treat Extrapyramidal syndrome:
due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
67
Buspirone
5HT1 Receptor Agonist
MOA: 5HT1A agonist
Use: anxiolytic drug; DOC for generalized anxiety
68
Pergolide
Ergot Alkaloid acting in the CNS
Used to treat hyperprolactinemia
69
Thioridazine
Phenothiazine typical antipsychotic
Causes retinal deposits-->browning of vision
Prolongs QT interval--> ventricular arrhythmias (patients taking enzyme inhibitors or other drugs that prolong QT interval)
MOA: D2 receptor antagonist
Schizophrenia: reduce + symptoms
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Tardive dyskinesias (occurs very late):
- oral/facial dyskinesias, muscle jerks, writhing lip muscles
- caused by relative cholinergic deficiency secondary to supersensitivty of DA receptors
- More common in pots taking typical antipsychotics
- Tx: switch patient to atypical drug (quetiapine or clozapine)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
Hyperprolactinemia: weight gain
70
Ketotifen
ORAL mast cell stabilizer used in prophylaxis of asthma, allergic rhinitis, allergic conjunctivitis
MOA: inhibits degranulation of mast cell by trigger stimuli
71
diphenhydramine
anti-muscarinic drug used to treat Extrapyramidal syndrome:
due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
72
Tegaserod
5HT4 Receptor Agonist
Use: IBS with constipation (stimulated release of ACh, increasing gastric motility)
73
Trifluoperazine
Phenothiazine typical antipsychotic
MOA: D2 receptor antagonist
Schizophrenia: reduce + symptoms
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Tardive dyskinesias (occurs very late):
- oral/facial dyskinesias, muscle jerks, writhing lip muscles
- caused by relative cholinergic deficiency secondary to supersensitivty of DA receptors
- More common in pots taking typical antipsychotics
- Tx: switch patient to atypical drug (quetiapine or clozapine)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
Hyperprolactinemia: weight gain
74
Omalizumab
Mast Cell Stabilizer used in prophylaxis of asthma
MOA: inhibits binding of IgE to mast cells and prevents the release of mediators (humanized monoclonal ab to human IgE
75
Clozapine
Atypical antipsychotic
MOA: 5-HT2 and D4 receptor antagonist, weak D2 affinity
Schizophrenia: reduce + symptoms and GREATER effect on negative symptoms
Causes agranulocytosis; weekly blood counts required
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
76
Drug to treat Tourette's
Haloperidol (typical antipsychotic)
77
Drug to treat manic episode in bipolar disorder
olanzapine and aripiprazole
78
Neurolept anesthesia
Droperidol + fentanyl + NO
79
Aripiprazole
Atypical antipsychotic
MOA: partial agonist at D2
Schizophrenia: reduce + symptoms; manic episode in bipolar disorder
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
80
Glucocorticoids
histamine release inhibitors
MOA: IgE dependent release
81
Antipsychotic that causes emesis and MOA
prochlorperazine
due to DA receptor blockade at the chemoreceptor trigger zone
82
Nedocromil
histamine release inhibitors
MOA: mast cell stabilizers--> prevents degranulation of mast cells
use: allergic asthma, allergic rhinitis, allergic conjunctivitis
83
Asenapine
Atypical antipsychotic
MOA: 5-HT2 and D4 receptor antagonist; weak D2 affinity
Schizophrenia: reduce + symptoms
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
84
Ketanserine
5HT2 Receptor Antagonist
MOA: 5HT2 and alpha receptor blocker
Use: topical preparation for glaucoma
85
Ergonovine
Ergot Alkaloid acting on the uterus
used to treat postpartum hemorrhage, IM
86
Cromolyn sodium
histamine release inhibitors
MOA: mast cell stabilizers--> prevents degranulation of mast cells
use: allergic asthma, allergic rhinitis, allergic conjunctivitis
87
Olanzapine
Atypical antipsychotic
MOA: 5-HT2 and D4 receptor antagonist; weak D2 affinity
Schizophrenia: reduce + symptoms; manic episode in bipolar disorder
Toxicity:
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
88
Beta 2 receptor agonist
histamine release inhibitors
89
theophylline
histamine release inhibitors
MOA: phosphodiesterase inhibitor
90
Olanzapine
5HT2 Receptor antagonist used to treat schizophrenia
91
Ergotamine
Ergot Alkaloid acting on the uterus and on the BV
used to treat postpartum hemorrhage, IM
also used to treat acute migraine
92
Gi receptor 2nd messengers
decreased cAMP
93
Risperidone
Atypical antipsychotic
MOA: 5-HT2 and D4 receptor antagonist; weak D2 affinity
Schizophrenia: reduce + symptoms
Toxicity:
Hyperprolactinemia (along with typical anti-psychotics) and weight gain
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
94
Lithium Carbonate
Inhibits the recycling of PIP2 --> depletion of 2nd messengers DAG and IP3
Used to treat acute mania or bipolar disorder (2-3 weeks for onset)
Prophylaxis of bipolar disorder when given with TCA
Low therapeutic index so plasma levels need to be monitored.
Contraindicated in pregnancy!
A/E:
- nausea
- vomiting
- diarrhea
- fine tremors
- polydipsia
- Nephrogenic DI (tx: amiloride)
- benign, reversible thyroid enlargement
Toxicity: confusion, drowsiness, ataxia, severe tremors
95
Gq receptor 2nd messengers
increased IP3 and DAG
96
Gs receptor 2nd messengers
increased cAMP
97
Alternate drugs to lithium
Carbamazepine and valproic acid
can be used alone or as adjuncts with lithium
98
Ziprasidone
Atypical antipsychotic
MOA: 5-HT2 and D4 receptor antagonist; weak D2 affinity
Schizophrenia: reduce + symptoms
Toxicity:
Prolongs QT interval--> ventricular arrhythmias (patients taking enzyme inhibitors or other drugs that prolong QT interval)
Extrapyramidal syndrome: due to dopamine receptor blockade of the nigro-striatal pathway:
- acute dystonia
- akathisias (agitation, distress, restlessness)
- parkinson like symptoms
--> treated by benztropine, biperiden, trihexphenyl, diphenhydramine (anti-muscarinic drugs)
Neuroleptic Malignant Syndrome: rare but life threatening
- caused by rapid blockade of post synaptic Da receptors
- m rigidity, alterations in BP and HR, hyperthermia, muscle-type CK elevated
- Tx: IV dantrolene
Adrenoceptor blockade:
- orthostatic hypotension
- reflex tachycardia
- impotence
- inhibits ejaculation
Muscarinic blockade:
- dry mouth, constipation, blurred vision, tachycardia, urine retention
99
Treatment for nephrogenic DI
Amiloride
100
H1 receptor type
Gq: increased IP3 and DAG
101
H2 receptor type
Gs: increased cAMP
102
H3 receptor type
Gi: decreased cAMP
103
H4 receptor type
Gi: decreased cAMP
104
H1 receptor located which organ
BV--> vasodilation--> decreased BP (by releasing NO)
bronchoconstriction --> features of anaphylaxis
H1 = increased IP3 and DAG
105
H2 receptor located in which organ
stomach --> stimulates gastric secretion
H2 = increased cAMP
106
H3 receptor located in which organ
presynaptic: brain, myenteric plexus, other neurons
H3 = decreased cAMP
107
H4 receptor located in which organ
eosinophils, neutrophils, CD4+ T cells
H4 - decreased cAMP
108
Cyproheptadine
5HT2 antagonist used to treat carcinoid tumors
109
Methysergide
Ergot Alkaloid acting on BV used to treat carcinoid tumor
110
NSAIDS used to treat acute migraine
- aspirin
- diclofenax
- ketorolac
- ibuprofen
- naproxen
All used to treat Mild or Moderate Migraine
111
Diphenhydramine
first generation H1 receptor antagonist
Use: allergic reactions, anaphylactic reactions
- and in treating drug-induced EPS
- anti-emetic action: motion sickness
A/E: sedation, peripheral and central anti-muscarinic actions, adrenoreceptor blocking actions.
112
Ondansetron
5HT3 receptor antagonist
MOA: central antiemetic action
Used to control vomiting associated with chemo
113
Drugs used to treat mild or moderate migraine
NSAIDS or Acetaminophen
114
Drugs used to treat moderate or severe migraine:
Ergot Alkaloids: Ergotamine; Ergotamine + Caffeine;
Triptans: Sumatriptan (all end in -triptan)
NSAIDs (aspirin, diclofenax, ketorolac, ibuprofen, naproxen)
Neuroleptics: Chlorpromazine and haloperidol
115
Chlorpheniramine
first generation H1 receptor antagonist
Use: allergic reactions, anaphylactic reactions
- and in treating drug-induced EPS
- anti-emetic action: motion sickness
A/E: sedation, peripheral and central anti-muscarinic actions, adrenoreceptor blocking actions.
116
beta blocker used in prophylaxis of migraine
propranolol
117
TCA used in prophylaxis of migraine
amitriptyline
118
Alosetron
5HT3 receptor antagonist used to treat IBS with diarrhea
119
Promethazine
first generation H1 receptor antagonist
Use: allergic reactions, anaphylactic reactions
- and in treating drug-induced EPS
- anti-emetic action: motion sickness
A/E: sedation, peripheral and central anti-muscarinic actions, adrenoreceptor blocking actions.
120
Ca Channel Blocker used in prophylaxis of migraine
flunarizine and verapamil
121
SSRIs used in prophylaxis of migraine
Fluxoetine
122
Anti-convulsant used in prophylaxis of migraine
sodium valproate
123
Serotonergic antagonist used in prophylaxis of migraine
cyproheptadine
124
Alprostadil
Eicosanoid; Type: PGE1
Use:
- cyanotic heart diseases: keeps DA open
- impotence
125
Hydrozyzine
first generation H1 receptor antagonist
Use: allergic reactions, anaphylactic reactions
- and in treating drug-induced EPS
- anti-emetic action: motion sickness
A/E: sedation, peripheral and central anti-muscarinic actions, adrenoreceptor blocking actions.
126
misoprostol
Eicosanoid; Type: PGE1
Use:
- NSAID-induced peptic ulcers
- combined with mifepristone (antiprogestin) --> induce abortion
127
Loratidine
second generation H1 receptor antagonist
NON-sedating!
Use: allergic reactions, anaphylactic reactions
128
Dinoprostone
Eicosanoid; Type: PGE2
Use: cervical ripening, abortifacient
129
fexofenadine
second generation H1 receptor antagonist
NON-sedating!
Use: allergic reactions, anaphylactic reactions
130
Carboprost
Eicosanoid; Type: PGF2a
Use: cervical ripening, abortifacient
131
cetirizine
second generation H1 receptor antagonist
NON-sedating!
Use: allergic reactions, anaphylactic reactions
132
Cimetidine
H2 receptor antagonist
MOA: competitive blockade of H2 receptors
- Inhibits p450
-causes gynecomastic bc blocks androgen receptors at hich doses
Uses:
- duodenal and gastric ulcer
- drug/stress induced ulcer
- GERD
- esophagits
- ZE syndrome
- dyspepsia
- heartburn
133
PGE2 synthesis blocker used to treat dysmenorrhea
NSAIDs
134
Latanoprost
Eicosanoid; Type: PGF2alpha
Use: glaucoma
135
ranitidine
H2 receptor antagonist
MOA: competitive blockade of H2 receptors
Uses:
- duodenal and gastric ulcer
- drug/stress induced ulcer
- GERD
- esophagits
- ZE syndrome
- dyspepsia
- heartburn
136
azelastin
second generation H1 receptor antagonist
NON-sedating!
Use: allergic reactions, anaphylactic reactions
137
epoprostenol
Eicosanoid; Type: PGI2
Use: pulmonary hypertension
138
famotidine
H2 receptor antagonist
MOA: competitive blockade of H2 receptors
Uses:
- duodenal and gastric ulcer
- drug/stress induced ulcer
- GERD
- esophagits
- ZE syndrome
- dyspepsia
- heartburn
139
5HT1A receptor
a) distribution
b) post-receptor mechanism
a) hippocampus, raphe nuclei
b) Gi: decreased cAMP
140
5HT1D receptor
a) distribution
b) post-receptor mechanism
a) cranial BV
b) Gi: decreased cAMP
141
5HT2A receptor
a) distribution
b) post-receptor mechanism
a) platelets, smooth muscle, CNS
b) Gq: decreased IP3, DAG
142
5HT3 receptor
a) distribution
b) post-receptor mechanism
a) area pastrami, sensory and enteric nerves
b) Na+/K+ ion channels
143
5HT4
a) distribution
b) post-receptor mechanism
a) NS and myenteric neurons, smooth muscle
b) Gs: increased cAMP
144
NO breakdown inhibitor
Sildenafil
145
NO donors
nitrates and sodium nitroprusside
146
used to treat diarrhea
diphenoxylate and loperamide
147
used to treat chronic malignant pain
via patches/lollipop
Fentanyl (or -fentanil derivatives) with droperidol
148
drugs used to precipitate opioid withdrawal
nalbuphine and pentazocine
149
Filgrastime
used to treat neutropenia caused by anti-cancer drugs
150
used to treat thrombocytopenia caused by anticancer drugs
IL-11 aka Oprelvekin
151
used to treat OD on fibrinolytic agents
aminocaproic acid-->
inhibits plasminogen activation
152
dipyridamole
phosphodiesterase III inhibitor
153
Flunitrazepam
used for date rape
154
sargramostim
used to treat neutropenia caused by anti-cancer drugs
155
drugs used to treat status epilepticus
via high dose IV
Phenobarbital, diazepam/lorazepam
156
Partial agonists at 5HT autoreceptors
buspirone and propranolol
157
fulmazenil
antagonizes effects of Zolpidem, Eszopiclone and Zaleplon
158
Ramelteon
agonist at melatnonin receptors
159
seizures caused by local anesthetics are treated by
Diazepam
160
Drug that inhibits xanthine oxidase
allopurinol
161
Methotrexate MOA
inhibits DHF reductase (inhibits folate metabolism)
So it's cytotoxic to immune cells
162
Azathioprine
purine anti-metabolite = immunosuppressor
163
Highly selective COX-2 inhibitors end in.... and are used to treat
-coxib
ie Celecoxib, Valdecoxib, Etoricoxib
Used to treat osteoarthritis and RA
164
Etanercept
monoclonal Ab against TNFalpha
highly effective and used to treat RA (s a disease-modifying RA drug)
165
Sulfasalazine
Disease-modifying RA drug
risk of allergic rxn if patients allergic to sulfur
5-aminosalycilic acid = anti-inflammatory active metabolite
166
N-acetylcysteine
Drug used to treat acetaminophen
MOA: replenishes glutathione stores in liver
Early symptoms of hepatic damage: nausea, vomiting, diarrhea, abdominal pain.
167
Salicylism and treatment
vomiting, tinnitus, decreased hearing, vertigo,
Reversible when treated with sodium bicarbonate
When higher doses of Aspirin are given
168
Quinidine
Class 1A anti-arrhythmatic-->these drugs slow conduction, cause prolonged QT interval
Primary: blocks voltage sensitive Na channels
Secondary: block inward rectifier K channels
binds to inactivated Na channels and prevents Na influx. slowing upstroke of Phase O
Toxicity:
- cinchonism: blurred vision, tinnitus, headache, disorientation and psychosis
- syncope
- prolonged QT
- torsades de pointes
169
Flecainide
Class 1C anti-arrhythmatic
170
Amiodarone
Class III anti-arrhythmatic
Block voltage gated K channel and diminish outward current during repolarization --> prolongs AP
Tx: refractory SVT and VT
Toxicity:
- thyroid dysfunction (affects peripheral conversion of T4-->T3)
- interstitial pulmonary fibrosis (pt needs routine CXR)
- corneal microdeposits
- blue-skin discoloration "surf skin"
- hepatotoxic (monitor liver enzymes)
171
Digoxin
decrased AV node conduction-->enhances vagal tone
use: Atrial Fibrillation and flutter
Toxicity: ectopic ventricular beats
used IV in emergencies
172
Sotalol
Class III anti-arrhythmatic
has strong anti-fibrillary effects in ischemic myocardium--> long-term therapy to decrease the rate of sudden death post-MI.
Prolongs both depolarization and duration of AP--> lengthens ERP
173
Magnesium
interferes with Na/K ATPase, Na channels, K channels, Ca channels
Used to treat Torsades de points (QT prolongation syndrome)
given slowly by IV and used with extreme caution!
174
Procainamide
Class 1A anti-arrhythmatic
Metabolism by acetylation to NAPA which PROLONGS DURATION OF AP (has properties of class III drugs)
Toxicity:
- reversible Lupus-like syndrome (in slow-acetylators)
- asystole
- ventricular arrhythmias
- depression
- hallucination
- psychosis
175
Adenosine
Decreases conduction velocity--> prolongs refractory period--> decreases SA and AV nodal activity by stimulating adenosine receptors
Toxicity: flushing, sedation, dyspnea
Used in IV for acute attacks due to its short half-life
176
drug that causes pulmonary fibrosis
amiodarone
177
drug that causes smurf skin
amiodarone
178
DOC in PSVT and AV nodal arrhythmias
Adenosine
179
Adenosine antagonists
Theophylline and caffeine
180
anti-arrhythmatic contraindicated in patients with cardiac failure
Dispyramide
Class 1A (slows conduction, prolongs QT interval) used to treat ventricular arrhythmias
181
H2 blockers
end in -tidine (cimetidine, ranitidine, famotidine, nizatidine)
Competitive inhibition
182
PPIs
end in -prazole (omeprazole, pantoprazole, lansoprazole, rabeprazole)
IRREVERSIBLY inhibit H/K atpase pump
183
Side effects of Sodium bicarbonate and calcium carbonate
bloating and metabolic alkalosis
184
drug interactions with antacids
tetracycline, fluroquinolones, iron salts
antacids decrease their absorption
185
Drug that causes blackening of stool, tongue and dentures
colloidal bismuth subsalicylate (ulcer protector, coats ulcer base)
186
Drugs used in triple therapy
2 antibiotics and a PPI for 14 days
amoxycillin
clarithromycin
tetracycline
metranidazole/tinidazole
187
Rifampicin
CYP inducer
188
CYP inhibitors
- cimetidine
- SSRIs
- ketoconazole
- macrolie antibiotics
- fluoroquinolones
- HIV protease inhibitors
- grapefruit juice
189
Sucralfate
Ulcer healing drug
polymerizes at Ph
190
barbiturates and phenytoin
CYP inducers
191
Leucovorin
foiling acid = active form of folic acid
192
Drugs that cause folate deficiency
- methotrexate
- phenytoin (CYP inducer and anti-convulsant)
- sulfonamides (antibiotics)
- INH
- OCPs
193
When do you give EPO?
anemic of chronic renal failure, chemotherapy or AIDs (i.e. zidovudine)
194
How do you treat acute iron poisoning
deferrioxamine (iron chelating agent)
195
factors that decrease Fe absorption
antacids, phosphate, phylates, tetracyclines and food
196
factors that increase Fe absorption
acids, amino acids, meat
197
When do you use folic acid
megaloblastic anemia, pregnancy
198
when do you use VB12
megaloblatic anemia, pernicious anemia
199
Meperidine
Opioid agonist
used to treat heroin withdrawal and pain of terminal cancer
causes tachycardia because of antimuscarinic action.
Also causes serotonin syndrome when combined with MAOIs (i.e. selegine rasagiline)
SS = muscle rigidity, myoclonus, diarrhea
also the exception, does NOT cause biliary colic
200
Treatment for opioid toxicity
Naloxone (rapid action) and Naltrexone
201
Buprenorphine
used in opioid dependence
202
LMWH all end in ....and MOA
LMWH all end in "-parin" (enoxaparin, dalteparin, tinzaparin)
Selectively inhibits Xa, less effect on thrombin
given subcutaneously. less side effects than heparin and better bioavailability
203
Hirudin
Anti-coagulant: Direct Thrombin Inhibitor
MOA: direction binds to thrombin and inhibits the downstream effects
used instead of heparin for anticoagulating patients with heparin-induced thrombocytopenia
204
Protamine
basic compound used to neutralize heparin
Toxicity: bleeding, thrombocytopenia, osteporosis
205
Anticoagulant that is Contraindicated in pregnancy
Warfarin
206
lepuridin
Anti-coagulant: Direct Thrombin Inhibitor
MOA: direction binds to thrombin and inhibits the downstream effects
used instead of heparin for anticoagulating patients with heparin-induced thrombocytopenia
207
Treatment for Warfarin toxicity
stop the drug, Vitamin K, fresh frozen plasma
Toxicity: bleeding, skin necrosis (rare)
208
Warfarin MOA
interferes with normal gamma carboxylation of VitK dependent clotting factors (including 7) by inhibiting Vit K epoxide reductase
given orally
209
Sinemet
DRUG used to treat Parkinsons DOPA preparation containing Carbidopa and levodopa
Carbidopa inhibita dopa decarboxulase --> increase L-dopa amounts in the brain
reduces symptoms of parkinson esp bradykinesia
210
bivalirudin
Anti-coagulant: Direct Thrombin Inhibitor
MOA: direction binds to thrombin and inhibits the downstream effects
used instead of heparin for anticoagulating patients with heparin-induced thrombocytopenia
211
Benzodiazepenes
end in "-azepam" "-azolam" or Chlordiazepoxide
212
Barbiturates
end in "-barbital" or thiopental
213
Bromocriptine
Used to treat Parkinson's
Dopamine receptor aconist--> increases dopamine levels
used for hyperprolactinemia
toxicity: nausea vomiting, postural HYPOtension and dyskinesia
214
argatroban
Anti-coagulant: Direct Thrombin Inhibitor
MOA: direction binds to thrombin and inhibits the downstream effects
used instead of heparin for anticoagulating patients with heparin-induced thrombocytopenia
215
Drugs that displace the protein binding of warfarin
aspirin, phenytoin, sulfonamides
216
drugs that inhibit the metabolism of warfarin
- CYP inhibitors (cimetidine, SSRIs, ketoconazole, macrolide AB, fluoquinolones, HIV protease inhibitors, grapefruit juice)
- antifungals
217
drugs that decrease Vitamin K production
antibiotics, cephalosporins
218
drugs that induce metabolism of warfarin
CYP inducers: barbiturates, rifampicin, phenytoin, glucocorticoids, chronic alcohol use, carbamazepine
219
Which anticoagulant is used for immediate anticoagulation
Heparin (activates antithrombin III; inactivates clotting factors in intrinsic pathway)
Toxicity: bleeding, thrombocytopenia, osteporosis
220
pramipexole
Used to treat Parkinson's
Dopamine receptor agonist-->increase dopamine levels
agonist at D3 receptor. Considered 1st line drug bc fewer side effects
toxicity: nausea vomiting, postural HYPOtension and dyskinesia
221
MAO-B inhibitor
Used to treat Parkinson's
end in -giline (selegiline, rasagiline)
Inhibition of enzymatic degradation of dopamine--> increased dopamine
use with Levodopa
can cause serotonin syndrome when combined with SSRIs or TCAs
Toxicity: insomnia, HYPOtension, GI distress, mood chnages,
When used with meperidine: agitation, delirium, death
222
COMT-inhibitor
Used to treat Parkinson's
Inhibition of enzymatic degradation of dopamine--> increased dopamine
end in -capone (entacapone, tolcapone)
Entacapone: doesn't cross BBB, peripheral effects only, preferred bc Tolcapone causes hepatic damage
Toxicity: dyskinesias, postural HYPERtension
223
Drug that may activate malignant melanoma
Levodopa (used to treat parkinson. Dopamine precursor)
also contraindicated in psychotic patients and those with angle-closure glaucoma
224
Amide Local Anesthetics
- Lidocaine (surface anesthetic)
- Bupivacaine (most cardiotoxic -->arrhythmias)
- mepivacaine
- etidocaine
- prilocaine (can cause black urine)
all are hepatic metabolized
225
Esther Local Anesthetics
- cocaine (DON'T give with EPI, causes vasoconstriction-->HTN, and used in nasal surgeries)
- procaine (short t 1/2)
- tetracaine
- benzocaine (surface anesthetic
226
Anti epileptics that block Na channels
- phenytoin
- carbamazepine
- topiramate
- phenobarbitone (also enhances GABA transmission
- valproic acid (also enhances GABA transmission and blocks T channels in the Thalamus)
- lamotrigine (also blocks gluamine receptors)
- Topiramate
227
DOC to treat GTC
phenytoin or Carbamazepine
228
Anti epileptics that Enhances GABA transmission
- phenobarbitone
- valproic acid
- diazepam
- clonazepam
- Vigabatrin (inhibits GABA transaminase)
- Tiagabine (interferes with GABA re-uptake)
- Topiramate
- Gabapentin (interferes with GABA reuptake)
229
Anti epileptics that block T channels
valproic acid, Ethosuximide, Valproate
230
DOC to treat simple partial and complex partial seizures
phenytoin, carbamazepine, valproate
231
DOC to treat absent seizures
Valproate, Ethosuximide, Clonazepam
232
DOC to treat febrile convulsions
diazepam
233
DOC to treat status epilepticus
Diazepam, lorazepam, phenytoin
234
DOC to treat bipolar disorder
Carbamazepine, valproate
235
DOC to treat seizures that develop after IV administration of lidocatine
Diazepam
also used to cause skeletal muscle relaxation
236
Temezepam
BZD used to treat insomnia
Works by increasing the frequency of GABA-mediated chloride channel openings
237
Alprazolam
BZD used to treat panic and phobias
Works by increasing the frequency of GABA-mediated chloride channel openings
238
IV anesthesia
diazepam, midazolam, lorazepam
Works by increasing the frequency of GABA-mediated chloride channel openings
239
ozazepam
BZD used to treat insomnia
Works by increasing the frequency of GABA-mediated chloride channel openings
240
Preferred agents to treat insomnia that cause no cognitive impairment
zolpidem
zolplone
eszopiclone
work by stimulating specific BZD receptors
241
Thiopentone
barbiturate used to induce GA
works by prolonging the duration of GABA-mediated chloride channel openings
242
Carbamazepine toxicity
- diplopia
- ataxia
- increased ADH secretion (dilution hyponatremia)
Carbamazepine = antiepileptic, and CYP enzyme inducer
243
Phenobarbitone toxicity
Phenobarbitone = antiepileptic and CYP enzyme inducer
- sedation
- drowsiness
- mood changes
244
valproic acid toxicity
= antiepileptic and CYP enzyme inhibitor
- neural tube defects
- hepatotoxicity in children
245
Phenytoin toxicity
= antiepileptic and CYP enzyme inducer
- gingival hyperplasia
- hirsutism
- nystagmus
- megalobalastic anemia
- osteomalacia
- teratogenia
- ataxia
- vertigo
- drowsiness
246
side effects of typical antipsychotics
- M block = dry secretions, constipation
- alpha block = postural hypotension, inhibition of ejaculation, reflex tachycardia
- H2 block = sedation
- D2 antagonism = hyperprolactinema (amenorrhea, galactorrhea, gynecomastia and impotence)
- D2 antagonism in nigrostriatal = EPS
247