B2 Drug Names Flashcards
Ibuprofen
Reversibly inhibits Cox 1 and 2
Succinylcholine
Depolarizing NM blocker
Baclofen
Spasmalytic: GABA B agonist
increased K flow–>hyper polarization–> reduces release of excitatory NT
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!!!
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
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
D- Tubocurarine
Competitive Nm blocker
Bile acid binding resins are contraindicated in whom?
patients with hypertriglyceridemia
Tizanidine
alpha 2 agonist used as a spasmolytic –> decreases m tone without causing paralysis
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!!!
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
Vecuronium
Competitive Nm blocker
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
Using what drugs along with statins causes an increased risk of myopathy?
- amiodarone
- verapamil
- fibrates
Dantrolene
Tx malignant hyperthermia
inhibits release of Ca from SR during excitation/contraction coupling
also inhibits ryanodine receptor and Calcium channels in skeletal m
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!!!
pancuronium
Competitive Nm blocker
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
How do you treat parities (itching) caused by Niacin?
aspirin or other NSAID
Gabapentin
spasmolytic
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
doxacurium
Competitive Nm blocker
Ezetimibe
HYPOlipidemic
reduces GI absorption of cholesterol–> reduces LDL and TG
Toxicity: diarrhea, abdominal pain
Vigabatrin
Anti-epileptic drug
MOA: irreversibly inhibits GABA transaminase (GTA)
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)
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
Rocuronium
Competitive Nm blocker
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)
Tiagabine
Anti-epileptic drug
MOA: blocks GABA reuptake by blocking GAT (GABA transporter)
Isoproterenol
Bronchodilator
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
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)
Levetriracetam
Anti-epileptic drug: treats GTC, simple partial seizures
MOA: binds to synaptic vesicular protein (SV2A) –> decreases synaptic release of glutamate
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
DOC for asthmatics on beta-blockeres
Ipratropium Bromide in combo with Salbutamol
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)
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
Felbamate
Anti-epileptic drug
MOA: Blocks NMDA (glutamate) receptors
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
Terbutaline
Bronchodilator
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
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
Gabapentin
Anti-epileptic drug
MOA: Binds to presynaptic voltage-gated N type of Ca channel –> decreases synaptic release of glutamate
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
Formeterol
Bronchodilator
MOA: sympathetic stimulation of Beta2 receptor (adrenergic agonist)
A/E: skeletal m tremor, tachycardia, palpitations tolerance (short acting drugs)
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
Pregbalin
Anti-epileptic drug
MOA: Binds to presynaptic voltage-gated N type of Ca channel –> decreases synaptic release of glutamate
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
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
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)
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
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
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)
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
Zonisamide
Anti-epileptic drug: tx myoclonic seizures
MOA: block high frequency firing via action on Na channels
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
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
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
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)
Typical Anti-psychotics:
end in “-zine” and haloperidol
Haloperidol
Typical Anti-psychotic;
used to treat touter’s syndrome and to reduce + symptoms in Schizophrenia
MOA: D2 receptor antagonist
Sodium Cromoglycate
Inhaled mast cell stabilizer used in prophylaxis of asthma, allergic rhinitis, allergic conjunctivitis
MOA: inhibits degranulation of mast cell by trigger stimuli
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
Sumatriptan
5HT1 receptor agonist
MOA: 5HT1D agonist
Use: acute migraine attack
Bromocriptine
Ergot Alkaloid that acts in the CNS
used to treat hyperprolactinemia and parkinson’s disease
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
Nedocromil
mast cell stabilizer used in prophylaxis of asthma, allergic rhinitis, allergic conjunctivitis
MOA: inhibits degranulation of mast cell by trigger stimuli
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
Buspirone
5HT1 Receptor Agonist
MOA: 5HT1A agonist
Use: anxiolytic drug; DOC for generalized anxiety
Pergolide
Ergot Alkaloid acting in the CNS
Used to treat hyperprolactinemia
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
Ketotifen
ORAL mast cell stabilizer used in prophylaxis of asthma, allergic rhinitis, allergic conjunctivitis
MOA: inhibits degranulation of mast cell by trigger stimuli
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
Tegaserod
5HT4 Receptor Agonist
Use: IBS with constipation (stimulated release of ACh, increasing gastric motility)
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
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
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
Drug to treat Tourette’s
Haloperidol (typical antipsychotic)
Drug to treat manic episode in bipolar disorder
olanzapine and aripiprazole
Neurolept anesthesia
Droperidol + fentanyl + NO
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
Glucocorticoids
histamine release inhibitors
MOA: IgE dependent release
Antipsychotic that causes emesis and MOA
prochlorperazine
due to DA receptor blockade at the chemoreceptor trigger zone
Nedocromil
histamine release inhibitors
MOA: mast cell stabilizers–> prevents degranulation of mast cells
use: allergic asthma, allergic rhinitis, allergic conjunctivitis
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
Ketanserine
5HT2 Receptor Antagonist
MOA: 5HT2 and alpha receptor blocker
Use: topical preparation for glaucoma
Ergonovine
Ergot Alkaloid acting on the uterus
used to treat postpartum hemorrhage, IM
Cromolyn sodium
histamine release inhibitors
MOA: mast cell stabilizers–> prevents degranulation of mast cells
use: allergic asthma, allergic rhinitis, allergic conjunctivitis
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
Beta 2 receptor agonist
histamine release inhibitors
theophylline
histamine release inhibitors
MOA: phosphodiesterase inhibitor
Olanzapine
5HT2 Receptor antagonist used to treat schizophrenia
Ergotamine
Ergot Alkaloid acting on the uterus and on the BV
used to treat postpartum hemorrhage, IM
also used to treat acute migraine
Gi receptor 2nd messengers
decreased cAMP
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
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
Gq receptor 2nd messengers
increased IP3 and DAG
Gs receptor 2nd messengers
increased cAMP
Alternate drugs to lithium
Carbamazepine and valproic acid
can be used alone or as adjuncts with lithium
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