PHARM 2 FINAL COMPLETE DRUG LIST

L-Dopa

MOA: Taken up by dopamine neurons and converted to dopamine

Primary indication: Treatment for Parkinson’s disease

Side effects/notes: Movement disorders from excess dopamine

Haloperidol

MOA: Dopamine antagonist on postsynaptic receptors

Primary indication: Treatment for schizophrenia/psychosis

Side effects/notes: Extrapyramidal side effects

Methylphenidate

MOA: Increase neurotransmitter release into synapse by blocking dopamine and norepinephrine transporters from recycling neurotransmitters (increases both dopamine and norepinephrine)

• Ritalin is immediate release form

• Concerta is extended-release form

Primary indication: Treatment for ADHD

Side effects/notes: Anxiety, irritability, insomnia, increase in blood pressure and heart rate

Amphetamine

MOA: Increase neurotransmitter release into synapse by blocking dopamine and norepinephrine transporters from recycling neurotransmitters (increases both dopamine and norepinephrine) It also leads to increase in DA availability by giving more dopamine back into the vesicles.

• Adderall is immediate-release form

• Vyvanse is extended-release form

Primary indication: Treatment for ADHD

side effects/notes: Anxiety, irritability, insomnia, increase in blood pressure and heart rate

• Vyvanse is only the D-form of amphetamine with a lysine attached; this is a “pro-drug”  so when it is broken down all you get is D-amphetamine, which is slowly released based on metabolism (Since Vyvanse is inactive until it is metabolized, the long-acting form limits abuse potential as taking short-acting doesn’t produce immediate effects)

Botulism toxin

MOA: Decrease the release of acetylcholine at the neuromuscular junction; without acetylcholine release, muscles cannot contract, leading to weakness and paralysis

Primary indication: Treatment for spasticity

Side effects/notes:

• Local injections for treatment of spasticity

• “Bladder botox” to treat overactive bladder

• Treatment of excessive drooling (sialorrhea) in conditions such as Parkinson’s or ALS

• Effect of local injection typically lasts 3-6 months 

Fluoxetine

MOA: SSRI (serotonin re-uptake inhibitor)

Primary indication: treatment for depression

Amitriptyline

MOA: Tricyclic antidepressant; blocks reuptake of both Serotonin and Norepinephrine

Primary indication: Treatment for anxiety/depression

Diltiazem

MOA: Calcium channel blocker

Primary indication: Hypertension

methadone

MOA: opioid agonist

primary indication: long-term agonist as treatment for opioid use disorder

side effects/notes: monitor OTc

Disulfiram

MOA: Inhibits acetaldehyde dehydrogenase; when someone takes alcohol while taking Disulfiram, you get build-up of acetaldehyde which causes flushing, vomiting, nausea

primary indication: Alcohol use disorder

side effects/notes: Patients may not want to take this daily as a preventative medication

Acamprosate

MOA: Interacts with glutamate and GABA transmission centrally to reduce cravings for alcohol

primary indication: Alcohol use disorder

side effects/notes: Renally excreted; contraindicated in low GFR

Naltrexone

MOA: Directly blocks opioid receptors and prevents euphoria associated with opioid abuse; also used in alcohol dependence (opioid system plays role in reinforcement behavior of alcohol use disorder)

primary indication: Alcohol use disorder/Opioid use disorder

side effects/notes: Metabolized in the liver; need to check liver function tests prior to starting

Buprenorphine

MOA: Partial opioid agonist

primary indication: opioid use disorder

Bupropion (Wellbutrin)

MOA: Blocks reuptake of norepinephrine and dopamine leading to increase in transmission (mechanism for action in depression)

primary indication: Nicotine dependence; depression

side effects/notes: Lower sexual side effects than SSRI or SNRI because it has minimal or no activity on serotonin receptors

Varenicline (Chantix)

MOA: Partial agonist at the α4β2 nicotinic acetylcholine receptors: mild stimulation of these receptors mimics nicotine’s actions

primary indication: Nicotine dependence

side effects/notes: Monitor for neuropsychiatric side effects

Guanfacine

MOA: Alpha 2A adrenoreceptor agonist;

• It acts on presynaptic alpha_2A-adrenoreceptors to decrease sympathetic nerve impulses via reduction in release of norepinephrine (NE)

• it also preferentially binds postsynaptic alpha_2A-adrenoreceptors in the prefrontal cortex and as a result increases connectivity in the dorsolateral prefrontal cortex (which has fewer connections in ADHD, given people have less “top-down” control of behavior)

primary indication: Treatment of ADHD

side effects/notes:

• Given it reduces sympathetic transmission, has mild sedative properties and can be useful with insomnia

• See monkey experiment below for more details on how Guanfacine works for ADHD

Modafinil

MOA: Multiple mechanisms (Dopamine and NE reuptake inhibitor), histamine stimulator

primary indication: Primary indication is treatment of narcolepsy; off label treatment of ADHD

ethanol

MOA: CNS depressant; potentiates actions of GABA; inhibits release of anti-diuretic hormone (ADH)

primary indication: Euphoria, impaired attention

treatment of intoxication: none

withdrawal treatment: Bezos

Amphetamine

MOA: Increase synaptic concentration of norepinephrine and dopamine (increases the amount of catecholamines packaged into vesicles)

primary indication: Euphoria, decreased fatigue, hypervigilance, Paranoia

treatment of intoxication: Lorazepam for agitation and Haldol for psychosis 

withdrawal treatment: supportive care

Methamphetamine

MOA: Increase synaptic concentration of norepinephrine and dopamine (increases the amount of catecholamines packaged into vesicles)

• Causes less norepinephrine release

primary indication: Euphoria, decreased fatigue, hypervigilance, Paranoia

treatment of intoxication: Lorazepam for agitation and Haldol for psychosis 

MDMA (Ecstasy)

MOA: Increases dopamine and serotonin in the brain (can have psychostimulant and psychotomimetic effects)

primary indication: Depersonalization, derealization, hallucinations, illusions

treatment of intoxication/withdrawal: supportive care

Cocaine

MOA: Inhibition of neuronal reuptake of norepinephrine and dopamine

primary indication: Euphoria, decreased fatigue, hypervigilance,

Paranoia

treatment of intoxication: Lorazepam for agitation or seizures  

treatment of withdrawal: supportive care

Caffeine

MOA: Produces mild stimulation by blocking adenosine receptors in neurons throughout the CNS

primary indication: Decreased fatigue, increased concentration

treatment of intoxication/withdrawal: supportive care

nicotine

MOA: Activates cholinergic nicotinic receptors in the central and peripheral nervous systems; also inhibits monoamine oxidase (leading to ability to activate dopaminergic neurotransmission and dependent properties)

primary indication: Tachycardia, increased concentration

treatment of intoxication/withdrawal: supportive care

Marijuana

MOA: Primary cannabinoid is THC. Binds to cannabinoid receptors in neurons

primary indication: Mild stimulation followed by depressive stage; can lead to impaired short-term memory

treatment of intoxication/withdrawal: supportive care

Lysergic acid diethylamide (LSD)

MOA: Selectively activates subtypes of serotonin (5-HT) receptors in the neocortex, limbic system and brainstem

primary indication: Visual hallucinations, synesthesia, little effect on cognitive function or arousal

treatment of intoxication/withdrawal: supportive care

Phencyclidine (PCP)

MOA: Dissociative anesthetic; blocks NMDA receptors

primary indication: Anxiety, delusions, emotional lability

Intoxication tx: Lorazepam for agitation and Haldol for psychosis 

 Withdrawal tx: Supportive care

Alprazolam (Xanax) 

MOA: Benzodiazepine; facilitates activity of GABA. Work only in the presence of GABA (therefor exhibits a ceiling effect)

primary indication: acute anxiety

side effects/notes:

• Can lead to dependence

• Caution in elderly

• Can lead to CNS depression; avoid with alcohol and other CNS depressants

Chlordiazepoxide (Librium)

MOA: Benzodiazepine; facilitates activity of GABA

primary indication: Alcohol detoxification given longer duration of action

side effects/notes:

• Can lead to dependence

• Caution in elderly

• Can lead to CNS depression; avoid with alcohol and other CNS depressants

Phenobarbital

MOA: Barbiturate; facilitates activity of GABA. Work independent of GABA, and do not exhibit ceiling effect (more prone to severe respiratory depression) 

primary indication: Seizure disorders

side effects/notes:

• Respiratory depression

• Induces Cytochrome P450 enzymes

Diphenhydramine (Benadryl)

MOA: Histamine antagonist

primary indication: Mild insomnia and anxiety disorders

side effects/notes: Anticholinergic side effects

Hydroxyzine

MOA: Histamine antagonist

primary indication: Mild insomnia and anxiety disorders

side effects/notes: Anticholinergic side effects and less sedating than benadryl

Zolpidem (Ambien)

MOA: Selectivity at targeting only GABA(A) receptors

primary indication: insomnia

side effects/notes: Shorter duration of action; fewer side effects and less dependence than Benzodiazepines

Buspirone

MOA: Partial agonist at Serotonin 5-HT1 receptors (causes up-regulation of postsynaptic serotonin receptors)

primary indication: Anxiety

side effects/notes: Used as a nonsedating anxiolytic drug

Carbamazepine

MOA: Blocks voltage-sensitive sodium channels (inhibits the spread of abnormal electrical discharges from the seizure focus)

primary indication: alternative to lithium in treatment of bipolar disease

side effects/notes: Potent inducer of cytochrome P450 enzymes

Phenytoin

MOA: Blocks voltage-sensitive sodium channels

primary indication: Seizure disorders

side effects/notes:  

• Inducer of CYP3A4 isoenzyme

• Can cause Stevens-Johnson syndrome

Phenobarbital

MOA: Enhances GABA-mediated chloride flux that causes membrane depolarization

primary indication: 2^nd line drug for seizure disorders

Valproic acid

MOA: Several mechanisms of action; overall increases GABA synthesis and decreases GABA degradation

primary indication: manic phase of bipolar disorder

side effects/notes: Serum levels must be monitored given extensive interactions with other drugs

Lamotrigine

MOA: Blocks voltage-sensitive sodium channels

primary indication: Treatment of partial seizures as well as manic phase of bipolar disorder

side effects/notes: Can cause Stevens-Johnson syndrome

Topiramate

MOA: several machanisms of actions

primary indications: Seizure disorders and weight loss

Gabapentin

MOA: GABA analog; increases release of GABA from central neurons

primary indications: Seizure disorders and post-herpetic neuralgia

side effects/notes: Can cause drowsiness at higher doses

HαM side effects:

Antihistamine =sedation, weight gain, delirium

α-antagonism = hypotension

Anti-muscarinic = dry mouth, blurry vision, urinary retention, delirium

Haloperidol (Haldol)

MOA: FGA; D2 antagonist

• D2 antagonism in the mesolimbic pathway represses positive symptoms of schizophrenia

• D2 antagonism in nigrostriatal pathway responsible for parkinsonian and other EPS symptoms

primary indications: Schizophrenia, severely agitated patients

side effects/notes: EPS symptoms

• EPS symptoms managed by Benztropine (anti-cholinergic), diphenhydramine (anti-histamine), and amantadine (increases dopamine release in basal ganglia)

Clozapine (Clozaril)

MOA: SGA; D2 antagonist and 5HT-2 antagonist

• Normally Serotonin leads to negative feedback on Dopamine release in mesocortical pathway. The 5HT-2 antagonist effect blocks negative feedback, leading to increase in Dopamine (thereby relieving negative symptoms of schizophrenia)

primary indications: Schizophrenia/psychosis 

side effects/notes: HAM” side effects

• Risk of agranulocytosis; need to frequently monitor WBC

Olanzapine (Zyprexa)

MOA: SGA; D2 antagonist and 5HT-2 antagonist

primary indications: Schizophrenia/psychosis

side effects/notes:

• “HAM” side effects

• Fewer autonomic side effects than Clozapine

• High risk of weight gain

Quetiapine (Seroquel)

MOA: SGA; D2 antagonist and 5HT-2 antagonist

primary indications:

• Low doses – used as a hypnotic

• Medium doses – Used as an anti-depressant

• High doses – Used as an anti-psychotic

side effects/notes: HAM side effects

Risperidone (Risperdal)

MOA:SGA; D2 antagonist and 5HT-2 antagonist

primary indications: Schizophrenia/psychosis

side effects/notes:

• Can increase Prolactin

• Most likely atypical to causes EPS

• Can also be used as injection (Invega)

Aripiprazole (Abilify)

MOA: Dopamine partial agonist

primary indications: Depression

side effects/notes: Can cause akathisia; overall not a great antipsychotic

Amitriptyline

MOA: TCA; blocks reuptake of norepinephrine and serotonin

primary indications: Depression

side effects/notes: Cause sedation (sometimes used to augment sleep)

Fluoxetine (Prozac)

MOA: Blocks reuptake of serotonin

primary indications: Depression, OCD, anorexia, bulimia

side effects/notes: effects than TCA’s

Sertraline (Zoloft)

MOA: Blocks reuptake of serotonin

primary indications: Depression

side effects/notes: Preferred in elderly patients (elimination not impacted by aging)

Venlafaxine

MOA: Blocks reuptake of norepinephrine and serotonin

primary indication: Depression

side effects/notes: Side effects similar to SSRI’s

Bupropion (Wellbutrin)

MOA: Many mechanisms; weak inhibitor of reuptake of dopamine, norepinephrine and serotonin. Sometimes labelled as “NDRI” because of effect at blocking Norepinephrine and Dopamine reuptake

• Antagonist at nicotinic cholinergic receptors

primary indications: Depression

side effects/notes: Can be “activating” and lead to weight loss; also used for smoking cessation

Mirtazapine (Remeron)

MOA: Blocks presynaptic alpha-2 auto receptors leading to increase of neuronal release of norepinephrine and serotonin

• Antagonist at 5HT-2 and 5HT-3 receptors 

primary indications: Depression/Insomnia

Lithium

MOA: Complex; overall reduces neuronal response to serotonin and norepinephrine

primary indication: Treatment of bipolar disorder (best treatment to control acute mania)

side effects/notes; Low therapeutic index, need to monitor lithium levels

Levodopa

MOA: Taken up by dopamine neurons and converted to dopamine

primary indication: Treatment for Parkinson’s disease

side effects/notes: Movement disorders from excess dopamine

Carbidopa

MOA: Structural analog to levodopa; reduces conversion of levodopa to dopamine in peripheral tissues, thereby increases the amount of levodopa that enters the brain

primary indications:Adjunct to Levodopa in treatment of Parkinson’s disease

side effects/notes: Reduces the GI and cardiovascular effects of Levodopa

Bromocriptine

MOA: D2 receptor agonist and D1 receptor antagonist

primary indications: Used as adjunct to Levodopa in patients with advanced Parkinson’s disease

Ropinirole

MOA: D2 receptor agonist

primary indications: Early stages of Parkinson’s disease; restless leg syndrome

Benztropine

MOA: Anticholinergic

primary indications: Adjunctive parkinsons treatment

side effects/notes: Anticholinergic side effects

Donepezil

MOA: Reversible cholinesterase inhibitor, which increases acetylcholine in the CNS

primary indications: Alzheimer’s disease

Penicillin G

MOA: Narrow-spectrum penicillin; activity against Strep species and enterococcus, erysipelas

primary indications: Syphilis, meningitis

Nafcillin

MOA: Penicillinase-resistant penicillin

primary indications: Osteomyelitis

Amoxicillin

MOA: Narrow-spectrum penicillin (An “aminopenicillin” – which has additional side chain to inhibit penicillin-binding protein);activity against Strep species and enterococcus

primary indications: Upper respiratory tract infections and otitis media

Augmentin (Amoxicillin/Clavulanate)

MOA: Extended-spectrum penicillin/Beta-lactamase inhibitor combination (Beta-lactamase inhibitor destroys beta-lactamase enzyme produced by bacteria)

primary indications: Upper respiratory tract infections caused by Haemophilus influenzae and Moraxella catarrhalis

Cephalexin

MOA: First-generation cephalosporin

primary indications: Skin and soft tissue infections (cellulitis)

side effects/notes: Does not have MRSA coverage

Ceftriaxone

MOA: Third-generation cephalosporin

primary indications: Gonorrhea, UTI’s, pneumonia

side effects/notes: Only available as IV therapy

Cefepime

MOA: Fourth-generation cephalosporin

primary indications:

• Used for drug-resistant Gram-negative infections (UTI, pneumonia)

• pseudomonas coverage

• no MRSA coverage

side effects/notes: Only available as IV therapy

Imipenem

MOA: Carbapenem

primary indications:

• Advanced infections that are multi-drug resistant

• no MRSA coverage

Bacitracin

MOA: Bacterial cell wall synthesis inhibitor

primary indications: Skin and eye infections;activity against strep and staph

side effects/notes: Topical treatment

Fosfomycin

MOA: Bacterial cell wall synthesis inhibitor

primary indications: Lower urinary tract infections; activity against Ecoli and enterococcus

side effects/notes:

• Does not achieve adequate concentrations anywhere else except the bladder, only use for mild UTI.  Long half-life allows for one time dose.

• Common treatment with one pill for UTI’s

Vancomycin

MOA: Bacterial cell wall synthesis inhibitor

primary indications: Bone and joint infections, activity against MRSA

side effects/notes: IV treatment needs blood monitoring with Vancomycin drug troughs 

Gentamycin

MOA: Aminoglycoside

primary indications:

• Aerobic gram-negative bacilli

• Pseudomonas coverage

side effects/notes:

• Aerobic gram-negative bacilli

• Pseudomonas coverage

Doxycycline

MOA: Tetracycline

primary indications: Gram-positive and gram-negative bacterial that cause respiratory tract infections and pneumonia

side effects/notes:

• Has activity against MRSA; can be used to treat MRSA cellulitis

• teeth discoloration

• nephotoxicity

• heptatoxicity

• phototoxicity

• all potential side effects of tetracyclines

Azithromycin

MOA: Macrolide

primary indications:

• Sinusitis, otitis media, bronchitis

• Effective single treatment for chlamydia

side effect: prolonged OTc

Erythromycin

MOA: Macrolide

primary indications: Topical treatment of conjunctivitis

Clindamycin

MOA: Macrolide 

primary indications:

• Activity against gram-positives and anaerobic organisms

• has MRSA coverage

side effects/notes:

• Associated with superinfections caused by Clostridium difficile

• Multiple day dosing to mitigate side effects

Mupirocin (Bactroban)

MOA: Inhibits bacterial protein synthesis

primary indications:

• Topical treatment of superficial infections

• impetigo

• folliculitis

Neomycin

MOA: Aminoglycoside (used in triple therapy alongside Bacitracin and Polymyxin)

primary indications: Topical treatment of superficial infections

side effects/notes: Most nephrotoxic aminoglycoside

Trimethoprim-sulfamethoxazole (Bactrim)

MOA: Anti-folate drugs with synergistic activity

primary indications: UTI’s, pulmonary infections caused by Pneumocystis jiroveci

• Has MRSA coverage

side effects/notes:

• Check renal function for dose-adjustment

• Monitor potassium for hyperkalemia

Ciprofloxacin

MOA: Fluoroquinolone

primary indications:

• Bacterial diarrhea

• UTI’s

• bone and joint infections

• pseudomonas coverage

side effects/notes:

• Black box warning from FDA causing tendonopathies

• Increased in elderly and young children

• Can cause delirium in elderly (caution use in those with dementia)

• QTc prolongation

• Decreases seizure threshold (caution use in those with epilepsy)

Levofloxacin

MOA: Fluoroquinolone

primary indication: Bronchitis/Community acquired pneumonia, UTI’s

side effects/notes:

• Black box warning from FDA causing tendonopathies

• Increased in elderly and young children

• Can cause delirium in elderly (caution use in those with dementia)

• QTc prolongation

• Decreases seizure threshold (caution use in those with epilepsy)

Nitrofurantoin (Macrobid)

MOA: Inhibition of bacterial enzymes

primary indications: Lower urinary tract (bladder) infections

side effects/notes: Only use for cystitis, does not have good tissue penetration. Dependent on renal function to get to the bladder (avoid use in CrCl<50 ml/hr)

Rifaximin

MOA: In treatment of hepatitis encephalopathy, decreases colonic bacteria and ammonia production

primary indications: Traveler’s diarrhea, hepatic encephalopathy

Metronidazole (Flagyl)

MOA: Inhibits DNA synthesis by causing strand breakage

primary indications: Treats gram positive and gram-negative organisms and anaerobes, primary indication is in treatment for Clostridium difficile

• CDiff first line is usually PO vancomycin

side effects/notes: Can be given PO or IV

Community acquired pneumonia (No comorbidities or risk factors for MRSA or Pseudomonas Aeruginosa)

Choose 1 agent

•       Amoxicillin 1gram TID

•       Doxycycline 100mg BID

•       Macrolides (Azithromycin)

Community acquired pneumonia (With Comorbidities (chronic heart diseases, lung, liver, or renal diseases)

Mono Therapy

•       Respiratory quinolones (Levofloxacin)

 

Combination Therapy

•       Beta-lactam PLUS Macrolide

•       Beta-lactam: Amoxicillin/clavulanate, cefpodoxime, cefuroxime

•       Macrolides: azithromycin

Community acquired pneumonia (Hospitalized)

Monotherapy and combination same as for CAP (outpatient)

 

Known colonization or prior infection with MRSA or high risk for MRSA: Add Vancomycin or Linezolid

Amphotericin B

MOA: Polyene antibiotic; Binds to fungal cell membrane and increases membrane permeability

primary indications: PO and IV treatment of systemic and subcutaneous fungal infections

side effects/notes: Ampho-terrible”

• Renal and other organ system toxicities

Nystatin

MOA: Polyene antibiotic; Binds to fungal cell membrane and increases membrane permeability

primary indications: Candida infections

side effects/notes: Oral or topical

Clotrimazole

MOA: Inhibits ergosterol synthesis

primary indications:

• Candida infections of mouth, throat, vagina and vulva

• Treatment of dermatophyte infections

side effects/notes: Oral and topical formulations

Fluconazole

MOA: Inhibits ergosterol synthesis

primary indications; Cryptococcal meningitis, patients with AIDS, vaginal candidiasis

sife effects/notes: Excellent penetration of the CSF

Ketoconazole

MOA: Inhibits ergosterol synthesis

primary indications: Seborrheic dermatitis

side effects/notes: Oral and topical formulations

Terbinafine

MOA: Inhibits ergosterol synthesis

primary indications: Onychomycosis (toe fungus)

side effects: Typically used orally when topical therapy has not been effective

Morphine

MOA: Opioid agonist

primary indications: Severe pain associated with trauma, myocardial infarction and cancer

side effects/notes:

• Undergoes considerable first-pass metabolism

• Metabolites can accumulate in renal failure

Methadone

MOA:  Opioid agonist & NMDA antagonist

primary indications: Opioid dependence or chronic pain

side effects/notes: Need to monitor QTc

Meperidine

MOA: Opioid agonist

primary indications: Obstetric or postsurgical analgesia

side effects/notes: Does not prolong labor as much as morphine

Oxycodone

MOA: Opioid agonist

primary indications:  Moderate or severe pain

side effects/notes: Long acting form is Oxycontin

Loperamide (Imodium)

MOA: Activates opioid receptors in gastrointestinal smooth muscle

primary indications: Diarrhea

Tramadol

MOA: Opioid agonist and serotonin and norepinephrine reuptake inhibitor

primary indications: Moderate pain

side effects/notes: Increased risk of suicidal thought and behaviors