Block 4 KISS quiz Flashcards
P450 Inducers
“St. Johns Pheny Pheny Mom Never Refuses Greasy Carbs or Chronic alcohol”
St.Johns wort
Phenytoin
Phenobarbital
Modanifil
Nevirapine
Rifampin
Griseofulvin
Carbamazepine
Chronic alcohol use
P450 Inhibitors
“SICKFACES.COM when i AM Really drinking Grapefruit juice”
Sodium Valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Acute alcohol overuse
Chloramphenicol
Erythromycin/Clarithromycin
Sulfonamides
Ciprofloxacin
Omeprazole
Metronidazole
Amiodarone
Ritonavir
Grapefruit juice
Acetylated drugs
“SHIPPD”
Sulfonamide
Hydralazine
INH
Procainamide & Penicillamine
Dapsone
Drugs involved in G6PD deficiency
“Hemolysis is D PAIN”
Isoniazid, sulfonamides, dapsone, primaquine,
aspirin, ibuprofen, nitrofurantoin
Macrolides
Azithromycin, clarithromycin, erythromycin
MOA:
MOR:
Clinical uses:
A/E:
MOA:
Binds S23rRNA of the 50S subunit
MOR:
Methylation of S23rRNA
Clinical use:
1) Atypical pneumonias
(Mycoplasma, Chlamydia, Legionella)
2) STIs (Chlamydia)
3) strep inf in penicillin allergic patients
4) B pertussis
A/E: “MACRO”
gi Motility issues
Arrythmia (prolonged QT)
acute Cholestatic hepatitis
Rash
eOsinophelia
TCA’s
Tetracycline, doxycycline, minocycline
MOR:
Clinical uses:
A/E:
MOA:
30S inhibitor (avoid milk)
MOR:
Efflux pumps
Uses:
1) Borrelia burgdorferi
2) M pneumoniae
3) Rickettsia
4) Chlamydia
5) community-acquired MRSA (Doxycycline)
A/E:
Teeth discoloration
Inhibited bone growth in kids
Photosensitivity
Aminoglycosides
Gentamicin, Neomycin, Amikacin,
Tobramycin, Streptomycin.
MOA:
MOR:
Clinical uses:
A/E:
MOA:
30S inhibitor
MOR:
Acetylation, phosphorylation or adenylation or bacterial transferase enzyme
Use:
1) Severe gram ⊝ rod infections
2) Neomycin for bowel surgery
A/E: “NNOT”
- Nephrotoxicity
- Neuromuscular blockade
(avoid in Myasthenia Gravis)
- Ototoxicity
- Teratogen
Tigecycline
MOA:
Clinical uses:
A/E:
MOA:
30S inhibitor
Use:
1) MDR (MRSA & VRE)
A/E:
N/V
Chloramphenicol
MOA:
MOR:
Clinical use:
A/E:
MOA:
50S inhibitor
MOR:
Plasmid encoded acetyltransferase
Use:
1) Meningitis
(Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae)
2) Rickettsial (Rocky Mountain spotted fever)
A/E:
Anemia & Aplastic anemia
Gray baby syndrome
Clindamycin
MOA:
Clinical use:
A/E:
MOA:
50S inhibitor
Use:
1) Aspiration pneumonia & lung abscesses
2) oral infections
3) Invasive group A streptococcal infection.
A/E:
Pseudomembranous colitis
(C difficile overgrowth)
Fever/Diarrhea
Linezolid
MOA:
MOR:
Clinical use:
A/E:
MOA:
50S inhibitor
MOR:
Point mutation in rRNA
Use:
Gram ⊕ species & MRSA and VRE
A/E:
Bone marrow suppression
Peripheral neuropathy
Serotonin syndrome
Polymyxins
Colistin (polymyxin E), polymyxin B
MOA:
Clinical use:
A/E:
MOA:
Makes cation polypeptides to disrupt cell membrane & cause leaks (cell death)
Use:
1) MDR ⊝ bacteria
(eg, P aeruginosa, E coli, K pneumoniae).
A/E:
Nephrotoxicity
Neurotoxicity
Respiratory failure
Vinca alkaloids
Vincristine, Vinblastine
MOA:
Clinical uses:
A/E:
MOA:
Inhibit microtubule formation (via binding B-tubulin)
Use:
Solid tumors
Leukemias,
Hodgkin/non-Hodgkin lymphomas
A/E:
Constipation & Neurotoxicity (Vincristine)
Myelosuppression (Vinblastine
Imatinib, dasatinib, & nilotinib
(-tinib)
MOA:
Clinical uses:
MOA:
Inhibits BCR-ABL tyrosine kinase → Prevents phosphorylation of proteins involved in cell cycle regulation.
Clinical uses:
CML, ALL, GISTs
A/E:
Myelosuppression
Increased LFTs,
Edema
Myalgias
Oseltamivir & Zanamivir
MOA:
Clinical uses:
MOA:
Inhibit influenza neuraminidase to reduce the release of progeny virus
Uses:
Treatment and prevention of influenza A and B. (within 48 hours)
Acyclovir, famciclovir, valacyclovir
MOA:
MOR:
Clinical uses:
A/E:
MOA:
Guanosine analogs
MOR:
Mutated viral thymidine kinase
Uses:
HSV & VZV
A/E:
Obstructive crystalline nephropathy & acute kidney injury if not hydrated
Acute management of asthma ?
Bronchodilators:
Salbutamol & Theophylline
Ipratropium & T
Ganciclovir
MOA:
MOR:
Clinical use:
A/E:
MOA:
Guanosine analog formed by a CMV viral kinase
MOR:
Mutated viral kinase
Uses:
CMV
A/E:
Bone marrow suppression
Renal toxicity
Foscarnet
MOA:
MOR:
Clinical uses:
A/E:
MOA:
Viral DNA/RNA polymerase inhibitor and
HIV reverse transcriptase
MOR:
Mutated DNA polymerase
Clinical uses:
CMV retinitis
Acyclovir-resistant HSV
A/E:
Nephrotoxicity
Electrolyte abnormalities
Seizures.
Cidofovir
MOA:
Clinical uses:
A/E:
MOA:
Inhibits viral DNA polymerase
Clinical uses:
CMV retinitis
Acyclovir-resistant HSV
A/E:
Nephrotoxicity (give with probenecid)
NRTIs
Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Tenofovir (TDF)
Zidovudine (ZDV,
formerly AZT)
MOA:
Clinical use:
A/E:
MOA:
Competitively inhibit reverse transcriptase
Use:
HIV
A/E:
Bone marrow suppression
Peripheral neuropathy
Lactic acidosis
Anemia (ZDV).
HLA-B*5701 mutation causes
hypersensitivity (Abacavir)
NNRTIs
Delavirdine
Efavirenz
Nevirapine
MOA:
Clinical use:
A/E:
MOA:
Bind to reverse transcriptase at site different
from NRTI’s
Use:
HIV
A/E:
Rash
Hepatotoxicity
CNS (Efavirenz)
Integrase inhibitors
Bictegravir
Dolutegravir
Elvitegravir
Raltegravir
MOA:
Clinical use:
A/E:
MOA:
Reversibly binds HIV integrase to prevent HIV genome from integrating into the host cell
Use:
HIV
A/E:
High creatine kinase
Protease inhibitors
Atazanavir
Darunavir
Lopinavir
Ritonavir
MOA:
Clinical use:
A/E:
MOA:
Prevent maturation of new viruses
Uses:
HIV
A/E:
Hyperglycemia
GI intolerance
Lipodystrophy (Cushing-like syndrome).
Entry inhibitors
Enfuvirtide VS Maraviroc
Enfuvirtide (Blocks FUSION)
MOA:
Binds gp41, inhibiting viral entry
A/E:
Skin reaction at injection sites.
Maraviroc (Blocks DOCKING)
MOA:
Binds CCR-5 on surface of T cells/monocytes,
inhibiting interaction with gp120
Amphotericin B
MOA:
Clinical use:
A/E: (“amphoterrible”).
MOA:
Binds ergosterol to tear holes in the
membrane pores causing leaks
Use:
Serious systemic mycoses.
1) Cryptococcus meningitis)
2) Blastomyces
3) Coccidioides meningitis.
4) Histoplasma
5) Candida & Mucor.
A/E:
Fever/chills (“shake and bake”)
Hypotension
Nephrotoxicity
Arrhythmias
Anemia
IV phlebitis
Nystatin
MOA:
Clinical use:
MOA:
Binds ergosterol to tear holes in the
membrane pores causing leaks
Use:
“Swish and swallow”
Oral candidiasis (thrush) or topical for Vaginal candidiasis
Flucytosine
MOA:
Clinical use:
A/E:
MOA:
Inhibits DNA and RNA synthesis by preventing conversion to 5-fluorouracil via cytosine deaminase
Clinical use:
Cryptococcus meningitis with Amphotericin B
A/E:
Bone marrow suppression
Azoles
Clotrimazole, fluconazole, isavuconazole, itraconazole, ketoconazole, miconazole, voriconazole
MOA:
Clinical use:
A/E:
MOA:
Inhibit ergosterol synthesis by inhibiting the cytochrome P-450 enzyme that converts
lanosterol to ergosterol
Use:
1) Chronic suppression of cryptococcal
meningitis in HIV (Fluconazole)
2) Blastomyces, Coccidioides, Histoplasma, Sporothrix schenckii (Itraconazole)
3) Topical fungal infections (Clotrimazole and
Miconazole)
4) Aspergillus & Candida (Voriconazole)
A/E:
1) Testosterone synthesis inhibition (gynecomastia, especially with ketoconazole)
2) liver dysfunction
(inhibits cytochrome P-450).
Terbinafine
MOA:
Clinical use:
A/E:
MOA:
Inhibits fungal squalene epoxidase.
Clinical use:
Dermatophytoses onychomycosis)
A/E:
GI upset, headaches, hepatotoxicity, taste disturbance.
Echinocandins
Anidulafungin, caspofungin, micafungin.
MOA:
Clinical use:
A/E:
MOA:
Inhibit cell wall synthesis by inhibiting synthesis of β-glucan
Use:
Invasive aspergillosis & Candida
A/E:
GI upset, flushing (by histamine release).
Griseofulvin
MOA:
Clinical use:
A/E:
MOA:
Interferes with microtubule function
Clinical use:
1) Dermatophytes (tinea, ringworm)
A/E:
Teratogenic, carcinogenic, confusion, headaches, disulfiram-like reaction, cytochrome P-450 and
warfarin metabolism
Antiprotozoal therapy for toxoplasmosis
Pyrimethamine (toxoplasmosis)
Antiprotozoal therapy for Trypanosoma brucei
suramin and melarsoprol (Trypanosoma brucei)
Antiprotozoal therapy for T cruzi
nifurtimox (T cruzi)
Antiprotozoal therapy for leishmaniasis
Sodium stibogluconate
Haloperidol
MOA:
Use:
A/E:
MOA:
D2 antagonist → Reduced dopamine neurotransmission.
Use:
Schizophrenia
Acute psychosis
Tourette syndrome
A/E:
EPS
Tardive dyskinesia
NMS
QT prolongation
Chlorpromazine
MOA:
Use:
A/E:
MOA:
D2 antagonist with anticholinergic effects.
Use:
Schizophrenia
Manic phase BPD
A/E:
Anticholinergic effects
Sedation
EPS
QT prolongation
Clozapine
MOA:
Use:
A/E:
MOA:
D2 and 5-HT2A antagonist
Use:
1) Treatment-resistant schizophrenia
2) Suicidality in schizophrenia/schizoaffective disorder.
A/E:
Agranulocytosis
Risperidone
MOA:
Use:
A/E:
MOA:
5-HT2A and D2 antagonist
Use:
Schizophrenia
BPD 1
Irritability in autism.
A/E:
EPS at higher doses
Hyperprolactinemia
QT prolongation.
Olanzapine
MOA:
Use:
A/E:
MOA:
5-HT2A and D2 antagonist with histaminergic & anticholinergic actions.
Use:
Schizophrenia
BPD 1
A/E:
Significant weight gain
Diabetes
Dyslipidemia.
Quetiapine
MOA:
Use:
A/E:
MOA:
5-HT2A and D2 antagonist with action on histamine and adrenergic receptors.
Use:
Schizophrenia
BPD
MDD
A/E:
Sedation
Weight gain
Less EPS risk.
Aripiprazole
MOA:
Use:
A/E:
MOA:
Partial agonist at D2 and 5-HT1A antagonist
Use:
Schizophrenia
BPD
MDD
Irritability associated with autism.
A/E:
Slight weight gain
Headache
Anxiety
Insomnia,
Acute dystonia
What is it?
How do you treat it?
within 4hrs
“MUSCLE”
Rigidity (without fever)
Treat with:
Benztropine (anticholinergic)
OR
Diphenhydramine or Chlorpheniramine
(H1 blockers)
Acute dystonia
What is it?
How do you treat it?
Within 4 days
Akathisia
“RUSTLE”
restlessness
Treat with propranolol (B-blocker)
Parkinsonism/Akinesia
What is it?
How do you treat it?
Within 4 weeks
HUSTLE
Akinesia, Bradykinesia (pin rolling)
Treat with:
Amantidine
Tardive Dyskinesia
What is it?
How do you treat it?
Within 4 months
Lip/tongue movements
Treatment:
Stop the antipsychotic & give an atypical drug
Benzodiazepines
Diazepam, Lorazepam, Alprazolam
MOA:
Use:
A/E:
Toxicity:
MOA:
Facilitate GABA(A) activity by increasing the frequency of Cl- channel opening → CNS depression
Use:
Anxiety
Seizures (especially status epilepticus)
Insomnia
Alcohol withdrawal
A/E:
Sedation, Dizziness, Ataxia, Cognitive dysfunction
Toxicity:
Flumazenil (GABA receptor antagonist)
Barbiturates
Phenobarbital, Thiopental, Pentobarbital
MOA:
Use:
A/E:
Toxicity:
MOA:
Facilitate GABA(A) activity by increasing the duration of Cl- channel opening → CNS depression
Use:
Sedation
Induction of anesthesia (Thiopental)
Seizure control (Phenobarbital)
Euthanasia
A/E:
Respiratory depression, Sedation, Dependence, CYP450 induction
Toxicity:
Sodium bicarbonate
Treatment of Tonic-Clonic Seizures:
Clinical Presentation: Characterized by sudden muscle rigidity (tonic phase) followed by synchronous muscle jerks (clonic phase), loss of consciousness.
1 Valproate
Phenytoin
Carbamazepine
Lamotrigine
Valproate
MOA:
Use:
A/E:
MOA:
Na+ channel inhibitor that inhibits GABA transaminase to increase GABA concentration
Use:
Tonic-Clonic, Absence, & Myoclonic seizures
Status Epilepticus
A/E:
Hepatotoxicity, Pancreatitis, Teratogenicity.
Phenytoin
MOA:
Use:
A/E:
MOA:
Na+ channel inhibitor
Use:
Tonic-Clonic & Partial/Focal seizures
A/E:
Gingival hyperplasia, Hirsutism, Teratogenicity, Ataxia.
Carbamazepine
MOA:
Use:
A/E:
MOA:
Na+ channel inhibitor
Use:
Clonic-Tonic & Partial/Focal seizures
A/E:
Bone marrow suppression, SIADH, Rash.
Lamotrigine
MOA:
Use:
A/E:
MOA:
Voltage-gated Na+ channel blockers that inhibit glutamate release and reduce neuronal excitability.
Use:
Tonic-Clonic & Partial/Focal seizures
A/E:
Stevens-Johnson syndrome.
Levetiracetam
MOA:
Use:
A/E:
MOA:
SV2A inhibitor SAFE IN PREGGOS
Use:
Partial/Focal seizures
Status epilepticus
A/E:
Behavioral changes, Psychosis.
Partial (Focal) Seizures
Clinical Presentation: Symptoms depend on the brain region involved; may have motor, sensory, autonomic, or psychic symptoms without loss of consciousness (simple partial) or with impairment (complex partial).
Treatment options
1Carbamazepine
Phenytoin
Lamotrigine
Levetiracetam
Absence seizures
Clinical Presentation: Brief, sudden lapses in attention and activity, often described as “staring spells.”
Treatment options?
1 Ethosuximide
Valproate
Ethosuximide
MOA:
Use:
A/E:
MOA:
T-type Ca2+ channels inhibitor
(in thalamic neurons)
Use:
Absence seizures
A/E:
GI distress, Fatigue, Headache.
Myoclonic Seizures
Clinical Presentation: Sudden, brief, involuntary muscle jerks.
Treatments?
1 Valproate
Levetiracetam (preggos)
Topiramate
Topiramate
MOA:
Use:
A/E:
MOA:
Voltage-dependent Na+ channels inhibitor that enhances GABA activity but antagonizes AMPA/kainate subtype of the glutamate receptor, and inhibits carbonic anhydrase
Use:
Myoclonic seizure
A/E:
Weight loss, Paresthesia, Cognitive slowing
Status Epilepticus
Clinical Presentation: A seizure lasting more than 5 minutes or two or more seizures within a 5-minute period without the person returning to normal between them.
Treatments?
1 Benzodiazepines (Lorazepam, Diazepam)
Phenytoin
Valproate
Levetiracetam
Esters
Procaine, Benzocaine (Note that these have one “i” in their generic name.)
MOA:
Uses:
A/E:
MOA:
Na+ channel inhibitors
Uses:
Procaine: Infiltration anesthesia, nerve block.
Benzocaine: Topical anesthesia for skin and mucous membrane.
A/E:
Allergy
Amides
Lidocaine, Bupivacaine, Ropivacaine (Note that these have two “i” in their generic name.)
MOA:
Uses:
A/E:
MOA:
Na+ channels inhibitor that get metabolized in the liver.
Uses:
Lidocaine: Topical, infiltration, nerve block, epidural, and IV for cardiac arrhythmias.
Bupivacaine: Epidural, spinal, and peripheral nerve blocks; longer duration than lidocaine
Ropivacaine: less cardiotoxicity; used for surgical anesthesia and pain management.
A/E:
1) CNS toxicity (e.g., seizures)
2) Cardiovascular toxicity
(arrhythmias & arrest)
NO
USE
PRO VS CON
A/E
Nitrous Oxide (NO)
MAC: ~105% (High MAC, Low Potency)
Advantages: Minimal cardiac effects, rapid onset and recovery.
Disadvantages: Low potency, must be used with other anesthetics.
Clinical Uses: Analgesia, minor surgical procedures.
HY S/E: Expansion of trapped gas in body cavities.
Halothane
USE
PRO VS CON
A/E
Halothane
MAC: 0.75%
Advantages: Potent with smooth induction.
Disadvantages: Hepatotoxicity, sensitization to catecholamines.
Clinical Uses: Mostly pediatric anesthesia.
HY S/E: Malignant hyperthermia, hepatotoxicity.
Isoflurane
USE
PRO VS CON
A/E
Isoflurane
MAC: 1.15%
Advantages: Potent, muscle relaxing, stable hemodynamics.
Disadvantages: Pungent, can cause respiratory irritation.
Clinical Uses: Maintaining anesthesia.
HY S/E: Mild respiratory irritation.
Desflurane
USE
PRO VS CON
A/E
Desflurane
MAC: 6.0%
Advantages: Very rapid onset and emergence.
Disadvantages: Airway irritation, requires special vaporizer due to high vapor pressure.
Clinical Uses: Rapid adjustment of anesthetic depth.
HY S/E: Coughing, laryngospasm, especially upon induction
Thiopental
USE
PRO VS CON
A/E
Thiopentone Sodium (Thiopental)
Clinical Uses: Induction of anesthesia, short surgical procedures.
Advantages: Rapid onset, short duration.
Disadvantages: Poor analgesic properties, respiratory and cardiovascular depression
.
HY S/E: Respiratory depression, hypotension.
Propofol
USE
PRO VS CON
A/E
Propofol
Clinical Uses: Induction and maintenance of anesthesia, sedation for procedures.
Advantages: Rapid onset and recovery, antiemetic properties.
Disadvantages: Pain on injection, respiratory and cardiovascular depression.
HY S/E: Propofol Infusion Syndrome (rare but serious).
Ketamine
USE
PRO VS CON
A/E
Ketamine
Clinical Uses: Induction of anesthesia, especially in patients with risk of hypotension and asthma.
Advantages: Preserves airway reflexes, stimulates heart rate and blood pressure.
Disadvantages: Emergence reactions (hallucinations), increased intracranial pressure.
HY S/E: Emergence reactions, increased secretions.
Opioids (e.g., Fentanyl)
USE
PRO VS CON
A/E
Opioids (e.g., Fentanyl)
Clinical Uses: Analgesia during and after surgery, component of general anesthesia.
Advantages: Potent analgesia, stable hemodynamics.
Disadvantages: Respiratory depression, nausea, pruritus.
HY S/E: Respiratory depression, risk of opioid addiction.
Benzodiazepines (e.g., Midazolam)
USE
CON
A/E
Benzodiazepines (e.g., Midazolam)
Clinical Uses: Pre-anesthetic sedation, induction of anesthesia, procedural sedation
.
Advantages: Anxiolysis, anterograde amnesia, muscle relaxation.
HY S/E: Sedation, amnesia.
Barbiturates (e.g., Phenobarbital)
Clinical Uses: Rarely used for anesthesia due to better alternatives; used in controlling certain types of seizures.
Advantages: Seizure control.
Disadvantages: Respiratory depression, cardiovascular effects.
HY S/E: Respiratory depression, dependency.
Malignant hyperthermia
What is it & how do you treat it?
Triggers: Certain anesthetics (e.g., halothane) and muscle relaxants (e.g., succinylcholine) can induce abnormal calcium release from the sarcoplasmic reticulum in muscle cells.
Clinical Features: Hyperthermia, Muscle Rigidity, Tachycardia, Acidosis, Hyperkalemia, Rhabdomyolysis (Breakdown of muscle tissue, releasing myoglobin into the blood.)
Treatment is DANTROLENE
(inhibits Ca2+ release from SR)
Neuroleptic Malignant Syndrome
What is it & what’s the treatment?
Presentation
1) Hyperthermia: Elevated body temperature.
2) Muscle Rigidity: “Lead pipe” rigidity, severe muscle stiffness.
3) Autonomic Dysregulation: Fluctuating blood pressure, tachycardia, diaphoresis.
4) Altered Mental Status: Confusion, agitation, delirium.
Trigger:
Antipsychotics → Dysregulation of dopamine pathways.
Treatment:
Discontinue the antipsychotic & give DANTROLENE & BROMOCRIPTINE OR AMANTADINE
Lithium
MOA:
Uses:
A/E:
Avoid which medications?
MOA:
Inhibition of phosphoinositol cascade → Reduced recycling of inositol phosphates and modulation of second messenger systems.
Uses:
BPD
Treatment-resistant depression
A/E:
Low hypothyroidism
Insipidus (diabetes)
Tremor (ataxia)
Heart (Epstein’s anomaly)
i
u
Nephrogenic
Drug-drug interaction: Avoid thiazide diuretics
(low Na+ cause lithium toxicity)
Selective Serotonin Reuptake Inhibitors (SSRI)
Fluoxetine, Sertraline, Citalopram
MOA:
Uses:
A/E:
MOA:
Inhibit serotonin (5-HT) reuptake
Uses:
Depression
Anxiety disorders (OCD, PTSD, PMDD)
Bulimia nervosa
A/E: “Sex, Stomach, & Sleep”
GI distress, Sexual dysfunction, Serotonin syndrome (with overdose or interaction), Mild anticholinergic effects, Sleep disturbance (insomnia)
Serotonin-Norepinephrine Reuptake Inhibitors (SNRI)
Venlafaxine, Duloxetine
MOA:
Uses:
A/E:
MOA:
Inhibits serotonin and norepinephrine reuptake
Uses:
Depression
GAD
Diabetic neuropathy (Duloxetine)
Chronic pain disorders
A/E: “Sex, Stomach, & Sleep”
GI distress, Sexual dysfunction, Increased blood pressure (especially Venlafaxine at high doses), Sleep disturbances
Tricyclic Antidepressants (TCA)
Amitriptyline, Nortriptyline, Clomipramine
MOA:
Use:
A/E:
MOA:
Block reuptake of norepinephrine (NE) and serotonin & block cholinergic, histamine, and alpha-1 adrenergic receptors
Use:
Depression
Neuropathic pain
Fibromyalgia
Migraine prophylaxis
OCD (Clomipramine)
A/E:
Anticholinergic effects
Orthostatic hypotension
Cardiotoxicity (arrhythmias)
Sedation
Weight gain
Monoamine Oxidase Inhibitors (MAOi)
Phenelzine, Tranylcypromine, Selegiline
MOA:
Use:
A/E:
MOA:
Phenelzine, Tranylcypromine:
Non-selectively inhibits monoamine oxidase (MAO) enzyme from breaking down NE, serotonin, and DA
Selegiline:
Selectively inhibits MAO-B at lower doses, affecting primarily dopamine breakdown.
Use:
Treatment-resistant depression
Atypical depression
Anxiety disorders
Parkinson’s disease (Selegiline)
A/E:
1) Hypertensive crisis (tyramine-rich foods)
2) CNS stimulation
3) Orthostatic hypotension
4) Weight gain
Selegiline-specific: Insomnia
Serotonin Syndrome
Triggers
Medications: SSRIs, SNRIs, MAOIs, TCAs, Triptans, St. John’s Wort, Illicit drugs (e.g., MDMA, LSD), and others when combined → Increase serotonin levels.
Diagnosis:
High levels of urinary 5-HIAA
What is it & what is the treatment?
confusion, agitation, headache, hallucinations, hyperthermia, rapid heartbeat, high blood pressure, sweating, nausea, diarrhea, tremors, muscle stiffness, and increased reflexes.
Treatment
Discontinue Serotonergic Agents
Cyproheptadine
(A serotonin antagonist → Reduces serotonin effects)
Cheese Reaction with TCAs leads to a Hypertensive crisis
What is the treatment?
1 Phentolamine
(A non-selective alpha-adrenergic blocker, can be used to counteract the vasoconstriction)
Nitroprusside: A vasodilator, for severe cases to rapidly reduce blood pressure.
Wilsons disease treatment (copper accumulation)
Penicillamine (copper chelator)
Pill-rolling” tremor
Resting Tremor: Often
“Lead pipe” rigidity
Bradykinesia
Postural Instability
Shuffling Gait
What’s the diagnosis?
What’s the 1st line treatment?
Other treatments?
1Levodopa/Carbidopa
Parkinsons
Others:
Dopamine Agonists (Pramipexole, Ropinirole)
MAO-B Inhibitors (Selegiline, Rasagiline)
COMT Inhibitors (Entacapone)
Anticholinergics (Benztropine)
Amantadine
Levodopa/Carbidopa (1st line)
MOA:
Use:
A/E:
MOA:
Increases brain dopamine concentrations
Use:
#1 Parkinsons
A/E:
Dyskinesias
‘on-off’ phenomena
neuropsychiatric effects.
Dopamine Agonists (Pramipexole, Ropinirole)
MOA:
Use:
A/E:
MOA:
Mimic dopamine at the receptor
Use:
Parkinsons
A/E:
Impulse control disorders, nausea, dizziness.
MAO-B Inhibitors (Selegiline, Rasagiline)
MOA:
Use:
A/E:
MOA:
Prevent dopamine breakdown.
Use:
Parkinsons
A/E:
Insomnia, nausea, risk of serotonin syndrome.
COMT Inhibitors (Entacapone)
MOA:
Use:
A/E:
MOA:
Prolong levodopa effect by reducing its metabolism.
Use:
Parkinsons
A/E:
Diarrhea, urine discoloration, dyskinesias.
Anticholinergics (Benztropine)
MOA:
Use:
A/E:
MOA:
Counteract excessive acetylcholine activity.
Use:
Parkinsons
A/E:
Dry mouth, blurred vision, constipation, confusion.
Amantadine
MOA:
Use:
A/E:
MOA:
May increase dopamine release and block NMDA receptors.
Use:
Parkinsons
A/E:
Livedo reticularis, ankle edema, confusion.
Memory Loss
Cognitive Decline
Behavioral Changes
Disorientation
Difficulty Recognizing Familiar People and Objects
What is the condition & the treatments?
Alzheimers
1) Cholinesterase Inhibitors
Donepezil, Rivastigmine, Galantamine
2) NMDA Receptor Antagonist
Memantine
Cholinesterase Inhibitors
Donepezil, Rivastigmine, Galantamine
MOA:
Uses:
A/E:
MOA:
Inhibit acetylcholinesterase
Uses:
Alzheimer’s
A/E:
Nausea, diarrhea, bradycardia, muscle cramps
NMDA Receptor Antagonist
Memantine
MOA:
Uses:
A/E:
MOA:
Regulates glutamate activity to prevent excitotoxicity, protecting nerve cells from excessive stimulation.
Uses:
Alzheimer’s
A/E:
Dizziness, headache, constipation, confusion
Progressive Neurodegenerative Disease: Affects motor neurons in the brain and spinal cord.
Key Symptoms: Muscle weakness, spasticity, difficulty speaking/swallowing, respiratory dysfunction
What is the condition & the treatments?
ALS
Treatments:
1) Riluzole
2) Baclofen
3) Edaravone
Riluzole
MOA:
Use:
A/E:
MOA:
Inhibits glutamatergic neurotransmission, which may help slow down neuronal damage.
Use:
ALS
A/E:
Dizziness, gastrointestinal disturbances, elevations in liver enzymes.
Baclofen
MOA:
Use:
A/E:
MOA:
GABA_B receptor agonist → Reduces muscle spasticity by inhibiting spinal reflexes
Use:
ALS
A/E:
Muscle weakness, drowsiness, fatigue, nausea.
Edaravone
MOA:
Use:
A/E:
MOA:
Acts as a free radical scavenger, reducing oxidative stress in neurons.
Use:
ALS
A/E:
Bruising, gait disturbances, headaches, skin irritation at the injection site.
ADHD
Characterized by: Inattention, hyperactivity, impulsivity
Treatment options:
1) Stimulants
Methylphenidate, Amphetamines (e.g., Adderall, Lisdexamfetamine)
2) Guanfacine (extended release)
3) Clonidine (extended release)
Stimulants
Methylphenidate, Amphetamines (e.g., Adderall, Lisdexamfetamine)
MOA:
Uses:
A/E:
MOA:
Increase dopamine and norepinephrine in the brain by inhibiting their reuptake and increasing their release.
Uses:
ADHD
A/E:
Insomnia, decreased appetite, weight loss, increased heart rate and blood pressure, potential for abuse.
Guanfacine (extended release)
Clonidine (extended release)
MOA:
Uses:
A/E:
MOA:
Alpha-2 adrenergic agonists → Reduce hyperactivity and improve attention by modulating prefrontal cortex activity
Uses:
ADHD
A/E:
Drowsiness, hypotension, fatigue, dry mouth.
Succinylcholine
MOA:
Uses:
A/E:
MOA:
Acts as a depolarizing neuromuscular blocker. It mimics acetylcholine at the neuromuscular junction, causing muscle cells to depolarize. The persistent presence of succinylcholine prevents repolarization, leading to paralysis.
Use:
Rapid sequence intubation (RSI)
Short surgical procedures
Emergency airway management
A/E:
Hyperkalemia
Malignant Hyperthermia (Dantrolene)
Bradycardia
MOR of penicillin’s
Beta lactamase
Mutated PBP
MOR of Vancomycin
Efflux pumps
Mutated Peptidoglycan cell wall
MOR of Quinolones
Mutated DNA gyrase
Efflux pumps
MOR of Aminoglycosides
Mutated ribosomal subunit
AG modifying enzymes
MOR of TCA’s
Efflux pump
MOR of Rifamycins
Mutated RNA polymerase
Methanol toxicity
Signs & Treatment?
Respiratory failure
Severe AG met acidosis
Ocular damage
Treatment:
Fomepizole
Acetaminophen toxicity
N-Acetylcysteine
Organophosphate toxicity
Atropine & Pralidoxime
Atropine toxicity
Physostigmine
Arsenic poisoning
Dimercaprol
Cyanide toxicity
Hydroxocobalamin & Sodium nitrite
Heparin toxicity
Protamine sulfate
TCA toxicity
Sodium bicarbonate
Morphine toxicity
Naloxone
Perioral tremor (“Rabbit syndrome”)
Perioral tremors Months-Years of antipsychotic therapy
Treatment:
Amantadine
Tamsulosin
MOA:
Use:
MOA:
α1 antagonist
Use:
BPH
Aromatase inhibitors
Anastrozole, letrozole, exemestane
MOA:
Use:
MOA:
Inhibit peripheral conversion of androgens to estrogen
Uses:
ER ⊕ breast cancer in postmenopausal females.
Selective estrogen receptor modulators
Clomiphene
MOA:
Uses:
MOA:
Antagonist at estrogen receptors in hypothalamus increasing the release of LH and FSH from pituitary, which stimulates ovulation.
Uses:
treat infertility (eg, PCOS)
Selective estrogen receptor modulators
Tamoxifen
MOA:
Uses:
A/E:
MOA:
Antagonist at breast, partial agonist at uterus, bone
Uses:
Treat and prevent recurrence
of ER/PR ⊕ breast cancer and to prevent gynecomastia in patients undergoing prostate cancer
A/E:
Risk of thromboembolic events
(especially with tobacco smoking), and endometrial cancer.
Selective estrogen receptor modulators
Raloxifene
MOA:
Uses:
A/E:
MO:
Antagonist at breast, uterus; agonist at bone
Uses: osteoporosis.
A/E:
Risk of thromboembolic events (especially
with tobacco smoking), but NO increased risk of endometrial cancer
Chronic gout
All painful flares are preventable.
Treatments?
Allopurinol
Pegloticase
Febuxostat
Probenecid
Sulfinpyrazone
Allopurinol
MOA:
Use:
MOA:
Competitive inhibitor of xanthine oxidase
Use:
Chronic gout
Pegloticase
MOA:
Use:
MOA:
Recombinant uricase catalyzing uric acid to
allantoin (a more water-soluble product)
Use:
Chronic Gout
Febuxostat
MOA:
Use:
MOA:
Inhibits xanthine oxidase. Think, “febu-xo-stat
makes Xanthine Oxidase static.”
Use:
Chronic gout
Probenecid
MOA:
Use:
MOA:
Inhibits reabsorption of uric acid in proximal
convoluted tubule. Can precipitate uric acid calculi.
Use:
Chronic gout
Acute gout drugs?
NSAIDs
Glucocorticoids
Colchicine
NSAIDs
MOA:
Uses:
MOA:
Any NSAID. Use salicylates with caution (may
decrease uric acid excretion, particularly at
low doses).
Use:
Acute gout
Glucocorticoids
MOA:
Uses:
MOA:
Oral, intra-articular, or parenteral.
Uses:
Acute gout
Colchicine
MOA:
Uses:
MOA:
Binds and stabilizes tubulin to inhibit
microtubule polymerization, impairing
neutrophil chemotaxis and degranulation.
Uses:
Acute gout
A/E:
1) GI & neuromyopathic side effects
2) Myelosuppression
3) Nephrotoxicity.
Mark the effects of these drugs:
Enfuvirtide
Zidovudine/Efavirenz
Oseltamivir
-gravir(s)
Amantadine
A: Enfuvirtide
B: Zidovudine/Efavirenz
C: Oseltamivir
D: -gravir(s)
E: Amantadine
Octreotide
MOA:
Use:
A/E:
MOA:
Long-acting somatostatin analog; inhibits secretion of various splanchnic vasodilatory hormones
Use:
Acute variceal bleeds
Acromegaly
VIPoma
Carcinoid tumors
A/E:
Nausea, cramps, steatorrhea. Risk of cholelithiasis due to CCK inhibition.
Loperamide
MOA:
Use:
A/E:
MOA:
Agonist at μ-opioid receptors; slows gut motility. Poor CNS penetration (low addictive potential).
Use:
Diarrhea
A/E:
Constipation, nausea.
Proton pump inhibitors
Omeprazole, lansoprazole, esomeprazole, pantoprazole, dexlansoprazole.
MOA:
Uses:
A/E:
MOA:
Irreversibly inhibit H+/K+ ATPase in stomach parietal cells
Uses:
Peptic ulcer
Gastritis
GERD
Zollinger-Ellison syndrome
H pylori
stress ulcer prophylaxis.
A/E:
Risk of C difficile infection
Pneumonia
Acute interstitial nephritis
Vitamin B12 malabsorption
HMG-CoA reductase inhibitors
Atorvastatin,
simvastatin
MOA:
Labs
A/E:
MOA:
Inhibit conversion of HMG-CoA to mevalonate, a cholesterol precursor;
Labs:
Very low LDL
high HDL
Low TG
A/E:
Hepatotoxicity ( LFTs),
myopathy (esp when
used with fibrates or
niacin
Niacin
MOA:
Labs
A/E:
MOA:
Inhibits lipolysis (hormone-sensitive lipase)
Labs
Very low LDL
Very high HDL
Low TG
A/E:
Flushed face
Hyperglycemia
Hyperuricemia
Fibrates
Gemfibrozil,
bezafibrate,
fenofibrate
MOA:
Labs
A/E:
MOA:
Activate PPAR-α
to upregulate LPL & TG
Labs:
Low LDL
High HDL
Very low TG
A/E:
Myopathy
Acute asthma treatment
Bronchodilator
Albuterol
Salmeterol, formoterol
ACE inhibitors have which levels
-PRIL
bradykinin
renin
AGT 1
AGT 2
Aldosterone
Increased bradykinin
High renin
High AGT 1
Low AGT 2
Low aldosterone
ARBS inhibitors have which levels
SARTANS
bradykinin
renin
AGT 1
AGT 2
Aldosterone
No change bradykinin
High renin
High AGT 1
High AGT 2
Low Aldosterone
Disulfiram-like reaction
Sorry pals, can’t go mingle
1st-generation sulfonylureas, procarbazine,
certain cephalosporins, griseofulvin,
metronidazole
Receptor Tyrosine Kinase
Insulin
Biguanides
Metformin
MOA:
Use:
A/E
MOA:
Increase insulin sensitivity VIA Inhibiting mGPD to inhibit of hepatic gluconeogenesis and the action of glucagon
Use:
Diabetes mellitus (2)
A/E:
GI upset, lactic acidosis (use with caution in
renal insufficiency), vitamin B12 deficiency.
Weight loss (often desired).
Loop diuretics
Furosemide, bumetanide, torsemide
MOA:
Uses:
A/E:
MOA:
Inhibit cotransport
system (Na+/K+/2Cl−) of thick ascending limb
of loop of Henle
Loops lose Ca2+
Uses:
Edematous states (HF, cirrhosis, nephrotic
syndrome, pulmonary edema)
Hypertension,
Hypercalcemia.
A/E: OHH DAANG
Ototoxicity, Hypokalemia, Hypomagnesemia,
Dehydration, Allergy (sulfa), metabolic
Alkalosis, Nephritis (interstitial), Gou
Acetazolamide
MOA:
Uses:
A/E:
MOA:
Carbonic anhydrase inhibitor, reduces NaHCO3 in the body
Uses:
Glaucoma
metabolic alkalosis
altitude sickness
intracranial hypertension.
A/E:
Proximal renal tubular acidosis
paresthesias, NH3
toxicity, sulfa allergy,
hypokalemi
Thiazide diuretics
Hydrochlorothiazide, chlorthalidone, & metolazone
MOA:
Uses:
A/E:
MOA:
Inhibit NaCl reabsorption in early DCT to reduce Ca2+ excretion
Uses:
Hypertension, HF, idiopathic hypercalciuria,
nephrogenic diabetes insipidus, osteoporosis
A/E:
Hypokalemic metabolic alkalosis,
hyponatremia, hyperglycemia, hyperlipidemia,
hyperuricemia, hypercalcemia. Sulfa allergy
Potassium-sparing
diuretics
Spironolactone, Eplerenone, Amiloride,
Triamterene.
MOA:
Uses:
A/E:
MOA:
Spironolactone and eplerenone are competitive aldosterone receptor antagonists in cortical collecting tubule
Triamterene and amiloride
block Na+ channels at the same part of the
tubule
Uses:
Hyperaldosteronism, K+ depletion, HF, hepatic
ascites (spironolactone), nephrogenic DI
(amiloride), antiandrogen (spironolactone).
A/E:
Hyperkalemia
gynecomastia, antiandrogen
Heparin
MOA:
Use:
A/D:
MOA:
Activates antithrombin, which reduce action primarily of factors IIa (thrombin) and Xa
Use:
Pulmonary embolism (PE)
Acute coronary syndrome
MI
DVT
(SAFE in Preggos)
A/D:
Bleeding (reverse with protamine sulfate), heparin-induced thrombocytopenia (HIT), osteoporosis
drug-drug interactions
Warfarin
MOA:
USE:
A/E:
MOA:
Inhibits vitamin K epoxide reductase by competing with vitamin K. Causes inhibition of vitamin K–dependent γ-carboxylation of clotting factors II, VII, IX, and X and proteins C and S.
Uses:
Chronic anticoagulation
(eg, venous thromboembolism prophylaxis and prevention of stroke in atrial fibrillation)
A/E:
Bleeding,
teratogenic effects,
skin/tissue necrosis A ,
drug-drug interactions (metabolized by
cytochrome P-450 [CYP2C9]).
Nitrates
Nitroglycerin, isosorbide dinitrate, isosorbide mononitrate
MOA:
Use:
A/E:
MOA:
Vasodilate by increasing NO in vascular smooth muscle to increase cGMP and smooth muscle relaxation.
Dilate veins»_space; arteries increases preload.
Use:
Angina, acute coronary syndrome, pulmonary edema.
A/E:
Reflex tachycardia (treat with β-blockers), hypotension, flushing, headache, “Monday disease”
Folic Acid
MOA:
Uses:
A/E:
MOA:
precursor of an essential donor of methyl groups used for synthesis of amnio acids, purines and deoxynucleotides
Uses:
folic acid deficiency (megaloblastic anemia), prevention of congenital neural tube defects
A/E:
can mask vitamin B12 deficiency in large amounts
Epoetin alfa (Erythropoietin)
MOA:
USES:
A/E:
MOA:
agonist of erythropoietin receptors expressed by red cell progenitors
USES:
anemias especially in chronic renal failure, HIV infection, cancer, prematurity –– prevention of need for transfusions
A/E:
hypertension, thrombotic complications, pure red cell aplasia
Enoxaparin
Classification: low-molecular weight heparin
MOA:
Use:
A/E:
MOA:
bind ATIII –– have same inhibitory effect on factor Xa as the unfractioned heparin-ATIII complex –– longer half-life than standard heparin
Use:
anticoagulation –– does not need laboratory monitoring (more predictable mechanism of action)
A/E:
ame as heparin, but less likely to experience thrombocytopenia and thrombosis
Contraindicated in renal failure
