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53 Cards in this Set

  • Front
  • Back
Treatment for Glaucoma
Treatments:
1. α agonists - ↓ aqueous humor SYNTHESIS
2. β blockers - ↓ aqueous humor SECRETION
3. Carbonic Anhydrase Inhibitor (Acetazolamide) - ↓ aqueous humor SECRETION (2° to ↓ HCO3)
4. Cholinomimetics - ↑ reuptake (outflow) of aqueous humor by contracting ciliary muscle and opening trabecular network to OPEN CANAL of SCHLEMM
5. Prostaglandin - ↑ outflow of aqueous humor
α agonists used to treat Glaucoma
Mech: ↓ SYNTHESIS of aqueous humor due to VASOCONSTICTION

Drugs: Epinephrine and Brimonidine

Side Effects of Epinephrine: Mydriasis and Stinging

C/I to Epinephrine: CLOSED-ANGLE GLAUCOMA
β blockers used to treat Glaucoma
Mech: ↓ SECRETION of Aqueous humor

Drugs: Timolol, Betaxolol, Carteolol
Acetazolamide in treatment of Glaucoma
Drug Class: Carbonic Anhydrase Inhibitor

Mech: ↓ HCO3 --> ↓ SECRETION of Aqueous Humor
Cholinomimetics used to Treat Glaucoma
Mech: CONTRACTS ciliary muscle and OPENS TRABECULAR NETWORK --> OPENING OF CANAL OF SCHLEMM. VERY effective

Drugs:
PILOCARPINE
PHYSOSTIGMINE
Carbachol
Echothiophate

Use PILOCARPINE in EMERGENCIES

Side Effects: Miosis, Cyclospasm (ciliary muscle used in accomodation to see objects at different distances)
Prostaglandin used to treat Glaucmoa
Mech: ↑ outflow of aqueous humor

Drug: Latanoprost
Drug used in emergencies for Glaucoma
PILOCARPINE
Opioid Analgesics
Morphine
Fentanyl
Codeine
Heroin
Methadone
Meperidine
Dextromethorphan
Mech: Act as agonists at opioid receptors
μ (morphine) receptors
δ (enkephalin) receptors
κ (dynorphin) receptors
Open K+ channels and close Ca2+ channels to HYPERPOLARIZE neurons and ↓ excitability

Use: Pain, Acute Pulmonary Edema, Cough Suppression (Dextramethorphan), Diarrhea (loperamide and diphenoxylate), and Addiction (Methadone)

Toxicities:
Addiction
Respiratory Depression
CNS Depression (additive with other drugs)
Miosis (pinpoint pupils)
Constipation

Reversal with Naloxone/Naltrexone (Narcan)
Opioid used to treat cough
DEXTROMETHORPHAN
Opioid used to treat heroin addiction
METHADONE
Butorphanol
Mech: Partial agonist at μ receptors, full agonist at κ receptors.

Use: Pain. LESS RESPIRATORY DEPRESSION

Toxicity: W/D if on full opioid agonist
Tramadol
Mech: very weak opioid agonist. inhibits SEROTONIN and NE reuptake. Multiple NTs = "Tram-it-all in"

Use: Chronic Pain

Toxicity: Similar to opioids
1st Line Therapy for Generalized Tonic-Clonic Seizures
Phenytoin
Carbamazepine
Valproic Acid (Valproate)
1st Line Therapy for Status Epilepticus PROPHYLAXIS
Phenytoin
1st Line Therapy for Abscence Seizures
Ethosuximide
1st Line Therapy for Partial or Generalized Seizures in PREGNANT WOMEN and CHILDREN
Phenobarbital
1st Line for ACUTE STATUS EPILEPTICUS
Benzodiazepines (Diazepam or Lorazepam)
1st Line for Seizures of Eclampsia
MgSO4

Often used in conjunction with Diazepam or Lorazepam
Used for Myoclonic Seizures
Valproate
Used for Partial, Generalized Tonic-Clonic, and PERIPHERAL NEUROPATHY
Gabapentin
Used for Seizures and TRIGEMINAL NEURALGIA
Carbamazepine
Phenytoin
Mech: Inactivation of Na+ channels
Use:
1st line for Generalized Tonic-Clonic Seizures
1st Line for Status Epilepticus PROPHYLAXIS
Partial Seizures
TYPE 1B ANTIARRHYTHMIC
Toxicities:
Nystagmus & Diplopia
Ataxia
Hirsutism
Megaloblastic Anemia
SLE-like Syndrome

Notes:
**INDUCER of Cyt P-450 --> ↓ concentration of drugs metabolized by Cyt P-450**
**TERATOGENIC - Minor Face and Limb Defects; MR, Variety of other defects**
Carbamazepine
Mech: Inactivation of Na+ channels

Use:
1st Line for Generalized Tonic-Clonic Seizures
1st Line for TRIGEMINAL NEURALGIA
Partial Seizures

Toxicity:
Diplopia
Ataxia
AGRANULOCYTOSIS
APLASTIC ANEMIA
Liver Toxicity

Notes:
**INDUCER of Cyt P-450 --> ↓ conc. of drugs metabolized by Cyt P-450**
**TERATOGENIC**
TERATOGENIC Seizure Treatments
PHENYTOIN
CARBAMAZEPINE
Valproic Acid
Mech: Inactivates Na+ channels AND ↑ GABA Concentration

Use:
1st Line for Generalized Tonic-Clonic Seizures
1st Line for Myoclonic Seizures
ABSENCE Seizures (not 1st line)
Partial Seizures

Toxicity:
NEURAL TUBE DEFECTS in Fetus
Rare but FATAL HEPTOTOXICITY
GI Distress
Weight Gain

C/I: PREGNANCY
Topiramate
Mech: Inactivation of Na+ channels AND ↑ action of GABA

Use:
Generalized Tonic-Clonic Seizures
Partial Seizures

Toxicity:
Kidney Stones (may shift away from this drug)
Sedation
Mental Dulling
Weight Loss
Lamotrigine
Mech: Inactivation of voltage-gated Na+ channels

Use:
Generalized Tonic-Clonic Seizures
Partial Seizures

Toxicity: Stevens-Johnson Syndrome (malaise, fever, purpuric rash that progresses to epidermal necrosis)
Gabapentin
Mech: ↑ release of GABA

Use:
Generalized Tonic-Clonic Seizures
PERIPHERAL NEUROPATHY
Partial Seizures

Toxicity: Sedation and Ataxia
Ethosuximide
Mech: Inactivates T-type Ca2+ channels

Use: Absence Seizures

Toxicity:
*Stevens Johnson Syndrome
*GI Distress
*Headache
Fatigue
Urticaria
Diazepam or Lorazepam
Mech: ↑ FREQUENCY of Cl- channels open due to GABA. Overall ↑ GABA action

Use:
1st Line for ACUTE STATUS EPILEPTICUS
Use with MgSO4 for Seizures of Eclampsia
Phenobarbital
Mech: ↑ DURATION of Cl- Channel opening due to GABA. Overall, ↑ GABA Action

Use:
1st Line Treatment for Seizures in PREGNANT WOMEN and CHILDREN (both Generalized Tonic Clonic and Partial)

Toxicity:
INDUCTION of Cyt P-450
Sedation
Dependence
Tolerance
Barbiturates
Phenobarbital
Pentobarbital
Thiopental
Secobarbital
Mech: ↑ DURATION that Cl- channels are open. ↑ action of GABA. ↓ Nerve firing

Use:
Sedative / Tx for Insomnia
Seizures
Induction of Anesthesia (Thiopental)

Toxicity:
Additive CNS depressant effects with other drugs (Alcohol)
CV or Respiratory Depression
INDUCTION of Cyt P-450
Dependence

Treatment of OD: Symptom Management (Assist Respiration, ↑ BP)
Benzodiazepines
Diazepam
Lorazepam
Midazolam
Triazolam
Alprazolam
Temazepam
Oxazepam
CHLORDIAZEPOXIDE
Mech: ↑ FREQUENCY of Cl- Channel Opening. ↑ Action of GABA and ↓ Neuron Firing.

Use:
1st Line for ACUTE STATUS EPILEPTICUS (diazepam/lorazepam)
Use with MgSO4 for Seizures of Eclampsia
Anxiety
↓ REM Sleep - Night Terrors, Sleepwalking
Detox from ETOH (DTs)

Toxicity:
Additive CNS Depressant effects with ETOH
Dependence

OD: FLUMAZENIL (competitive antagonist)

Note: LESS risk of RESPIRATORY DEPRESSION than Barbiturates
Inhaled Anesthetics
Halothane
Isoflurane
Desflurane
Enflurane
Sevoflurane
NITROUS OXIDE
Mech: Unknown

Effects:
Myocardial and Respiratory Depression
↑ cerebral blood flow (∴ ↓ cerebral demand)
Nausea/Emesis

Toxicities
Malignant Hyperthermia - Rare, but serious. Tx: Dantrolene
Halothane - Hepatotoxicity
Enflurane - Proconvulsant
Methoxyflurane - Nephrotoxicity
Nitrous Oxide - Expansion of Trapped Gas
IV Anesthetics (5)
Barbiturates (Thiopental)
Benzodiazepines (Midazolam)
Ketamine
Opiates
Propofol
Thiopental
Barbiturate IV Anesthetic

Characteristics: ↑ Potency, (↑ Lipid Solubility); Rapid Onset and Recovery (↓ Blood Solubility)

Use: Induction of Anesthesia & Short Procedures

Toxicity: ↓ Cerebral Blood Flow
Midazolam
Benzodiazepine IV Anesthetic

Characteristics: Used with Gaseous anesthetics and Narcotics

Use: Most common drug for endoscopy

Toxicity:
SEVERE Post Op Respiratory Depression
↓ BP
Amnesia (Beneficial)
Ketamine
PCP Analog used as a Dissociative IV Anesthetic

Mech: Blocks NMDA receptors (glutamate).

Use: IV anesthesia (kids)

Toxicity:
Cardiovascular stimulant
Disorientation, Hallucinations, Bad Dreams
NO RESPIRATORY DEPRESSION
Opiates used as IV Anesthetics
Fentanyl and Morphine

Used in conjunctions with other IV anesthetics
Propofol
IV Anesthetic

Mech: Potentiates GABA

Use: Rapid anesthesia induction and short procedures

Note: LESS Post Op NAUSEA than with THIOPENTAL
Succinylcholine
Mech: DEPOLARIZING PARALYTIC (Neuromuscular Blocking Drug). Selective for Motor Nicotinic Receptors.

Use: Muscle Paralysis in surgery or Mechanical Ventilation

Toxicity: ↑ K, ↑ Ca

2 Phases:
Phase I: Prolonged depolarization. No Reversal. WORSE with AChEsterase INHIBITORS
Phase II: repolarized but blocked. REVERSAL with Cholinesterase inhibitors (neostigmine, physostigmine).
Vecuronium // Pancuronium // Rocuronium // Atracurium // TUBOCURARINE
Mech: NON-DEPOLARIZING PARALYTICS. Competitive Inhibitors at Acetylcholine (ACh) Receptors

Reversal: AChE Inhibitors (neostigmine, physostigmine, Edrophonium)
Dantrolene
Mech: Prevents Ca2+ release from sarcoplasmic reticulum of sk. muscle.

Use: Malignant Hyperthermia (caused by inhaled anesthetics + Succinylcholine) AND Neuroleptic Malignant Syndrome (similar to Malig. Hyperthermia)
Parkinson's Disease Pharm Strategy
1. Agonize Dopamine Receptors (Bromocriptine)

2. ↑ Dopamine (L-Dopa & Carbidopa // Amantadine)

3. Prevent Dopamine Breakdown (Selegiline // Entacapone or Tolcapone)

4. ↓ Cholinergic Activity (Benztropine / Other Antimuscarinic)

BALSA
B = Bromocriptine
A = Amantadine
L = L-dopa / Carbidopa
S = Selegiline
A = Antimuscarinics (Benztropine)
Bromocriptine // Pramipexole // Ropirinole
Mech: Dopamine Receptor Agonist

Use: Parkinson's to simulate effect of dopamine

Side Effects: Compulsive Gambling, Disinhibition
Levodopa / Carbidopa
Mech: Levodopa is L-Dopa (unlike dopamine, it can cross BBB). Dopa Decarboxylase converts to Dopamine in CNS. Carbidopa is a COMT inhibitor that prevents decarboxylation of L-Dopa in the periphery.

Use: ↑ amount of Dopamine in CNS

Side Effects:
Long Term Use:
dyskinesia with administration
akinesia in between administrations
Treatment of Familial / Essential Tremor
β-BLOCKERS!
Amantadine
Mech: may ↑ Dopamine RELEASE

Use:
Parkinson's
Antiviral - Influenza A and Rubella

Toxicity: Ataxia
Selegiline
Mech: Selectively Inhibits MAO-B (↑ Dopamine availability)

Use: Parkinson's Disease

Toxicity: May enhance Adverse Effects of L-Dopa
Benztropine
Mech: Antimuscarinic

Use: Parkinson's for Tremor and Rigidity, but NOT USEFUL FOR BRADYKINESIA

**Essentially Peripheral Symptom Management**
Sumatriptan
Mech: Serotonin (5-HT 1B & 1D) Agonist causing vasoconstriction, inhibiting trigeminal activation and vasoactive peptide release.

Use: Acute Migraine and Cluster Headaches

Toxicity: Coronary VASOSPASM

C/I: CAD or Prinzmetal's Angina
Memantine
Mech: NMDA Receptor Antagonist. Prevents Excitotoxicity (Ca2+ mediated)

Use: Alzheimer's

Toxicity: Dizziness, Confusion, Halucinations
Donepezil
Mech: Centrally Acting AChE Inhibitor

Use: Alzheimer's

Toxicity: Nausea, Dizziness, Insomnia