Shared Flashcard Set

Details

Pharm, Ass7
Anesthesia, Migraines, Derm
147
Pharmacology
Graduate
10/06/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Nitrous Oxide
Definition

Inhalation Anesthetic; comes in vapor form, cheaper - "vapor sparing";

Analgesia (not full anesthetic) and anesthesia;

Allows maintenance of protective reflexes;

 

Less respiratory depression and less CV effects than other inhalational anesthetics.

 

SE - potential teratogen, N/V (more than many anesthetics) drowsiness, dizziness, vertigo, dysphorya, panic, amnesia, laughing (laughing gas), parasthesias, B12 synthetase inhbitor.

Term
Halothane
Definition

Liquid Inhalation Anesthetic;

3rd (of 3) agent of choice (last line);

Has a high blood:gas partition coefficient and is very lipid soluble (requires a lot to get CNS effects).

Is converted in part to metabolites (instead of all being exhaled) and metabolites are hepatotoxic.

 

SE - arrhythmias (esp w/ CA), hepatotoxicity (halothane hepatitis - an immune reaction occurs when halothane metabolites bind liver components causing liver damage), loss of reflexes, hypoventilation, CV depression

Term
Enflurane
Definition

Liquid Inhalation Anesthetic;

2nd (of 3) agent of choice;

 

SE - areflexia, irritant, muscle relaxation, SEIZURES, hepatic tox, hypoventilation, CV depression

Term
Isoflurane
Definition

Liquid Inhalation Anesthetic;

'1st' agent of choice;

 

SE - areflexia, irritant, muscle relaxation, hypoventilation

Term
Desflurane
Definition

Liquid Inhalation Anesthetic;

'1st' agent of choice - newer;

Accumulates and equilibrates quickly,

PLUS rapid recovery;

 

SE - areflexia, irritant, hypoventilation

Term
Sevoflurane
Definition

Liquid Inhalation Anesthetic;

'1st' agent of choice - newer;

Accumulates and equilibrates quickly,

PLUS rapid recovery;

 

SE - areflexia, hypovent, CV depression

Term
Thiopental
Definition

Induction agent (IV anesthetic);

Barbiturate - prolongs binding of GABA to GABA receptor; Shifts endogenous GABA curve L;

NO analgesic activity;

 

SE - Respiratory depression, bronchospasm, interactions lead to CV effects, coma/death

Term
Methohexital
Definition

Induction agent (IV anesthetic);

Barbiturate - prolongs binding of GABA to GABA receptor; Shifts endogenous GABA curve L;

NO analgesic activity;

 

SE - Resp depression, bronchospasm, interactions lead to CV effects, coma/death

Term
Propofol
Definition

Induction agent (IV anesthetic);

↑ GABA activity, ↓ Glutamate activity,

 

RAPID action; NO analgesia;

Sedation, antiemetic (obviously has mch lower incidence of N/V than other anesthetics), ↓ ICP;

 

SE - ↓ CBF, CO, RR, Propofol Infusion Syndrome

Term
Etomidate
Definition

Induction agent (IV anesthetic);

↑ GABA's action, may displace endogenous antagonists;

 

Potent cerebral vasoconstrictor;

Good drug for pt with CV problems;

 

SE - injection pain, inhibits steroidogenesis (↓ HPA axis), ↓ CBF; no prolonged use (actually not used in ICU either).

Term
Ketamine
Definition

Inhibits Glutamate NMDA receptor, specific CNS depression;

Balanced anesthesia; IV and IM;

Potent analgesic,

Stimulates Sympathetic NS, bronchodilates;

Triggers a dissociated state (eyes can remain open but no pain and no consciousness);

 

SE - hallucinations (Angel Dust effects, use short acting BZ to control after sedation), ↑ CBF, ↑ MAP, ↑ CO

Term
Diazepam
Definition

(Valium)

Benzodiazepine - balanced anesthesia;

↑ activity of GABA receptor/channel;

No analgesia;

Long duration of action (20-40 hr);

PO;

Anticonvulsant, anterograde amnesia, balancing sympathomimetic effects;

Benzo is often given PO the night before surgery (sedation, anxyolysis)

Wide safety margin;

SE - prolonged sedation, long 1/2 life;

(Flumazenil = specific BZ antagonist)

Term
Lorazepam
Definition

(Ativan)

Benzodiazepine - balanced anesthesia;

↑ activity of GABA receptor/channel; 

No analgesia;

Intermediate duration of action (15 hrs), PO or IM;

 

Anticonvulsant, anterograde amnesia, balancing sympathomimetic effects;

 

Wide safety margin;

(Flumazenil = specific BZ antagonist)

 

 

Term
Midazolam
Definition

Benzodiazepine (IV) - balanced anesthesia;

↑ activity of GABA receptor/channel; 

No analgesia;

 Short duration of action (3hrs); IM or PO;

 

Anticonvulsant, anterograde amnesia, balancing sympathomimetic effects;

Wide safety margin;

(Flumazenil = specific BZ antagonist)

Term
Lidocaine
Definition

Local anesthetic - Amide (hepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

MC used form;

Rapid onset, intermediate duration;

 

ALSO... in RSI is used to ↓ ICP and bronchospastic response

 

SE: Rarely, Lidocaine OD can present as unconsciousness.

Term
Mepivacaine
Definition

Local anesthetic - Amide (hepatic metabolism);

Injectable (no topical effects);

 

Blocks Na channels, ↑ refractory period;

 

Slow onset, intermediate duration;

 

Term
Prilocaine
Definition

Local anesthetic - Amide (hepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 

Rapid onset, intermediate duration; 

↓ acute tox;

 

SE - Methemoglobinemia (Ferric Hb, cyanosis)

Term
Bupivacaine
Definition

Local anesthetic - Amide (hepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 

Slow onset, LONG duration;

Very potent due to long binding, useful for post-op analgesia.

 

SE - Cardiotoxicity (binds Na+ channels in the heart), inadvertant trauma to the tounge/mouth (pt can't feel!)

Term
Ropivacaine
Definition

Local anesthetic - Amide (hepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 

Slow onset, LONG duration; Very potent due to long binding;

 

SE - Less cardiotoxicity/greater safety margin than Bupivacaine.

Term
Procaine
Definition

Local anesthetic - Ester (extrahepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 

Slow onset, short duration;

 

Standard used to measure potency (lowest potentcy)of other agents;

 

SE - Esters have a slightly increased incidence of allergic reaction (coverted to para-aminobenzoic acid during metabolism).

Term
Chloroprocaine
Definition

Local anesthetic - Ester (extrahepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 

Rapid onset, SHORTEST duration (1/2 life);

Minimal fetal exposure

Term
Tetracaine
Definition

Local anesthetic - Ester (extrahepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 

Slow onset, long action;

HIGH POTENCY; Potentially very toxic

Term
Cocaine
Definition

Local anesthetic - Ester (extrahepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

 

Topical ENT use;

Causes potent vasoconstriction;

 

SE - cardiac arrhythmias (esp w/ epi), ischemia and gangrene in nasopharynx

Term
Articaine
Definition

Local anesthetic - ester and amide!;

Thiophene rather than benzene as the aromatic group;

Injectable;

Blocks Na channels, ↑ refractory period;

Fast onset, intermediate duration;

Rapidly metabolized to an inactive product;

 

Dental use w/ epi; Good penetration into BONE;

 

SE - PARASTHESIAS

Term
Benzocaine
Definition

TOPICAL local anesthetic;

Causes swelling of membrane, occlusion of Na channels;

 

Often for Mucous membranes (contra to Nagel, unique aspect of this among the topical local anesthetics);

 

SE - methemoglobinemia

Term
Dyclonine
Definition

TOPICAL local anesthetic;

Blocks Na channels, ↑ refractory period;

Found in Cepacol and Sucrets (soothes sore throats!)

 

Often for Mucous membranes (contra to Nagel, unique to this and Benzocaine among topical local anesthetics);

Term
Dibucaine
Definition

TOPICAL local anesthetic;

Blocks Na channels, ↑ refractory period;

 

Skin use, NOT mucus membranes (contra to Nagel);

Term
Promoxine
Definition

TOPICAL local anesthetic;

Blocks Na channels, ↑ refractory period;

 

Skin use, NOT mucus membranes (contra to Nagel);

Term
ELMA
Definition

Common ER prep;

Topical local anesthetic mixture;

 

Prilocaine + Lidocaine; apply, wrap, wait, wipe, proceed

Term
TAC
Definition

Commonly used in pediatric ERs;

Tetracaine + Adrenalin (epi) + Cocaine;

Topical local anesthetic; Liquid formulation;

 

Effective when applied through LASCERATED SKIN;

No effect on non-cut skin but is rapidly absorbed through mucous membranes if it gets there.

Term
Phentolamine
Definition

alpha-1,2 Antagonist;

Used to reverse the actions of local anesthetics by causing vasodilation;

Gets local anesthetics away from the area and reverses their effects.

Term
Lipid rescue
Definition
Infusion of lipid emulsion to treat severe cardiotoxicity (et. al) of local/regional anesthetics
Term
Promethazine
Definition

(Phenergan)

H1, dopamine and cholinergic receptor Antagonist;

Anti-emetic; Anti-dopaminergic, anti-cholinergic;

 

Tx: peri-op sedation, anti-emetic tx N/V in migraine pt;

 

SE -  threshold for seizures (↓ use bc of this effect), respiratory depression, glaucoma, BPH

 

Comes in a preparation with the opiate Butorphanol (mixed ag/antag) to mitigate the opiate SE of ↑ N/V

Term
Hydroxyzine
Definition

H1 antagonist;

  POand IM;

 

SEDATIVE,

anticholinergic, antiemetic

Term
Diphenhydramine
Definition

(Benadryl)

H1 anti-histamine (CNS actions);

PO and IM;

 

SEDATIVE, ANTICHOLINERGIC, antiemetic

Term
Cimetidine
Definition

(Tagamet)

H2 antagonist;

"No" CNS sedation;

Pre-op ancillary agent for anesthesia;

 

Will neutralize the pH of gastric acid secretions but has no effect on pre-existing acid level/content

Term
Ranitidine
Definition

(Zantac)

H2 antagonist;

"No" CNS sedation;

Pre-op ancillary agent for anesthesia;

 

Will neutralize the pH of gastric acid secretions, no effect on pre-existing acid level/content

Term
Bicitra
Definition

Non-particulate Antacid;

Na- and K-citrate + citric acid;

 

Neutralizes existing contents of stomach (pre-op drug)

 

*It is better to use a non-particulate antacid when possible (rather than a particulate like Riopan, Rolaids, or Tums) because, should aspiration occur, non-particulates do less damage to the lungs.

Term
Polycitra
Definition

Non-particulate Antacid;

Na- and K-citrate + citric acid;

 

Neutralizes existing contents of stomach

Term
Metoclopramide
Definition

Gastrokinetic/anti-emetic;

PO and IV;

Centrally acting D2 antagonist = anti-emetic, sedation; Sensitizes upper GI to Ach (antagonized by anticholinergics and narcotics*);

Accelerates gastric emptying and peristalsis;

 

 Tx: Pre-op prep of gastric contents + anti-emetic in tx N/V in migraine sufferers;

 

SE -  seizure threshold*, 

↑ prolactin secretion (gynecomastia), drowsiness, confusion, alters bioavaliliblity of oral drugs (alters absorption dynamics), and can potentiate the extra-pyramidial effects of other drugs.

Term
Ondansetron
Definition

(Zofran)

Serotonin (5-HT3) receptor antagonist;

 

Anti-emetic; Expensive, reserved for severe cases

Term
Cefazolin
Definition

Antibiotic,

Prophalyxis of infection;

 

Ancillary drug to anesthesia;

 

Tx STAPH AND STREP

Term
Cefotetan
Definition

Antibiotic, prophalyxis of infection;

Ancillary drug to anesthesia;

 

Tx: infection with BOWEL ANEROBES

Term
Cefoxitin
Definition

Antibiotic, prophalyxis of infection;

Ancillary drug to anesthesia;

 

Tx infection with BOWEL ANEROBES

Term
Vancomycin
Definition

Antibiotic, prophalyxis of infection;

Ancillary drug to anesthesia;

 

Reserve use for when MRSA is suspected,

Routine use is discouraged.

Term
Atropine
Definition

Anticholinergic;

Strong Vagolytic effects (tx bradycardia, ↑ hr);

Pre-op ancillary agent for anesthesia;

 

Tx reflex bradycardia, blocks muscarinic anticholinesterases (NM blocker OD); prevents drying of secretions;

ALSO... In Rapid Seq Intubation- counteracts bradycardia in response to succinylcholine, esp in children <10yrs

Term
Glycopyrrolate
Definition

Anticholinergic;

*Anti-sialogogue effect (dry secretions);

Pre-op ancillary agent for anesthesia;

 

Tx: Reflex bradycardia, blocks muscarinic anticholinesterases (NM blocker OD); prevents the drying of secretions

Term
Scopolamine
Definition

Anticholinergic;

*Sedation and amnesia;

Pre-op ancillary agent for anesthesia;

 

Tx reflex bradycardia, blocks muscarinic anticholinesterases (NM blocker OD), prophylaxis for the drying of secretions; Blocks pathways from inner ear (anti-emetic, tx motion sickness)

Term
Vecuronium
Definition

Rapid sequence intubation-

Decreases fasciculations and mitigates ICP response to Succinylcholine

Term
Fentanyl; non analgesic action
Definition

Rapid Sequence Intubation;

↓ sympathetic response to procedure;

 

Indicated if ↑ ICP, hemorrhage, CV dz

Term
Dopamine
Definition

Ancillary: post-op CV support;

 

Tx hypoT;

Has a beta effect on heart and maintains renal perfusion

Term
Phenylephrine
Definition

(AK-Dilate)

Ephedrine can also be used, same indications/SE*

Pressor/sympathomimetic: alpha-agonist;

Ancillary: post-op CV support; 

 

Tx hypoT;

Term
Nitroprusside
Definition

Ancillary: post-op CV support;

vasodilation, venodilation

 

Tx: Post-op HTN (short-acting is all that is needed because most post-op HTN lasts < 4 hrs)

Term
Trimethaphan
Definition
Ancillary: post-op CV support;
tx HTN;
Dec sympathetic tone - vasodilation;
Prevention of reflex tachy
Term
Epinephrine think Post-op
Definition

Ancillary: tx post-op Anaphylaxis;

Initial* agent given to stimulate CV=vasoconstriction;

 

Interactions with beta blockers, TCAs, Halothane.

 

Consider another agent if pt has:

Closed angle glaucoma, HTN, coronary dz, arrhythmia, diabetes, hyperthyroidism, heart failure (CHF), or a cerebrovascular disorder.

Term
Aminophylline
Definition

Ancillary: tx post-op Anaphylaxis;

 

2ndary use; tx persistent bronchospasm related to admin of Succinylcholine

Term
Hydrocortisone
think Post-op
Definition
Ancillary:
tx post-op Anaphylaxis;
Anti-inflamm function of LT, PGs, kinins released by mast cells
Term
Methylprednisolone
Definition

Ancillary: tx post-op Anaphylaxis;

 

Blunts the anti-inflammatory effects of LT, PGs, kinins released by mast cells

Term
Propofol Infusion Syndrome
Definition

Iatrogenic dz;

Acidosis, rhabdomyolysis, arrthymias, heart and kindey failure;

 

Risk factors - dec O2 delivery, prior cerebral injury;

 

Tx - Remove the agent, CV stabilization, correct acidosis.

Term
NSAID and Migraine
Definition

(review) 1st treatment - mild to moderate migraine;

Act to ↓ PG synthesis which ultimately ↓ MAPK in the nerver terminal which ↓ production of CGRP and SP (↓ inflammatory mediators)

 

SE - gastric irritation, nephrotoxicity (dec renal blood flow); CI - G6PD deficiency and high dose aspirin

Term
Butalbital
Definition

Barbituate for acute migraine tx;

Binds the GABAA receptor at it's alpha subuint to enhance GABA action in the thalamus - sedative;

 

SE - Strongly assoc with Analgesic Overuse Syndrome, CYP450 inducer, CNS and respiratory depressant;

 

CI: In pt with Porphyria,

In pt drinking ethanol or taking sedatives*

 

Availible for tx migraines in combination products with ASA/Acetaminophen and Caffeine.

Term
Butorphanol
Definition

Opiate for acute migraine tx;

Agonist/antagonist of all 3 ORs, action particularily in the thalamus and higher centers;

 

SE - respiratory depression, bradycardia, histamine release, QT prolongation, constipation, CYP3A4's, N/V

Term
Acute therapy of migraines review (5) agents
Definition

NSAIDs

Opiates

Triptans

Ergot's

(Anti-emetics)

Term
Naratriptan
Definition

Triptan

1st line tx for mod/severe acute migraine;

5-HT1B & 1D agonists - Cerebral vasoconstriction, inhibits trigeminal n activation/trigeminal cervical complex activation; 

Metabolized by CYP450 but does not give rise to active metabolites = most favorable adverse event profile;

 

Least problems with triptan interaction

SE - Sleepiness, difficulty thinking, ↑HR, dizziness, coronary and peripheral vasospasm*

 

Absolutely CI: in pt with coronary/peripheral vascular dz, uncontrolled HTN or ischemic bowel dz, OR in pt taking Ergot alkaloids (additive vasospastic effects).

Term
Rizatriptan
Definition

Triptan

1st line tx for mod/severe acute migraine;

5-HT1B & 1D agonists - Cerebral vasoconstriction, inhibits trigeminal n activation/trigeminal cervical complex activation; 

Metabolized by CYP450/MAO;

 

SE - Sleepiness, difficulty thinking, ↑HR, dizziness, coronary and peripheral vasospasm*

 

Absolutely CI: in pt with coronary/peripheral vascular dz, uncontrolled HTN or ischemic bowel dz, OR in pt taking Ergot alkaloids (additive vasospastic effects).

Term
Sumatriptan
Definition

(Imitrex) Triptan

 

1st line tx for mod/severe acute migraine;

 

5-HT1B & 1D agonists - Cerebral vasoconstriction, inhibits trigeminal n activation/trigeminal cervical complex activation; 

 

Does not cross the BBB* (somehow effects are transmitted to the CNS, Metabolized by CYP450/MAO;

 

 

 

SE - Sleepiness, difficulty thinking, ↑HR, dizziness, coronary and peripheral vasospasm*

 

 

 

Absolutely CI: in pt with coronary/peripheral vascular dz, uncontrolled HTN or ischemic bowel dz, OR in pt taking Ergot alkaloids (additive vasospastic effects).

 

Term
Zolmitriptan
Definition

Triptan

1st line tx for mod/severe acute migraine;

5-HT1B & 1D agonists - Cerebral vasoconstriction, inhibits trigeminal n activation/trigeminal cervical complex activation; 

 

Metabolized by CYP450/MAO;

 

SE - Sleepiness, difficulty thinking, ↑HR, dizziness, coronary and peripheral vasospasm*

 

Absolutely CI: in pt with coronary/peripheral vascular dz, uncontrolled HTN or ischemic bowel dz, OR in pt taking Ergot alkaloids (additive vasospastic effects).

 

Term
Dihydroergotamine (DHE)
Definition

Ergot for acute SEVERE migraine tx;

Agonist on 5-HT1&2, α1&2, D2;

Central and peripheral vasoconstriction; Unpredictible effects on BP (may need a concurrent α antag);

 

SE - drug interactions (CYP3A4), Category X teratogen, can cause valvular heart dz;

 

CI - w/ any vasospastic condition (CAD or peripheral), with Triptans, vasoconstrictors, tobacco, or propranolol. With CYP3A4 inhibitors (SSRI, HIV drugs, Azole antifungals)

Term
Ergotamine
Definition

Ergot for acute SEVERE migraine tx;

Agonist on 5-HT1&2, α1&2, D2;

Central and peripheral vasoconstriction; Unpredictible effects on BP (may need a concurrent α antag);

 

SE - drug interactions (CYP3A4), Category X teratogen, can cause valvular heart dz;

 

CI - w/ any vasospastic condition (CAD or peripheral), with Triptans, vasoconstrictors, tobacco, or propranolol. With CYP3A4 inhibitors (SSRI, HIV drugs, Azole antifungals)

Term
Prochlorperazine
Definition

Anti-emetic use in acute tx of Migraines;

Central D2 blockade at chemoreceptors + Ach and α-adrenergic blockade;

 

SE - Sedation, dyskinesia, hypoT, glaucoma, additive CNS effects, ↓ seizure threshold

Term
Chlorpromazine
Definition

Anti-emetic use in acute tx of Migraines;

Central D2 blockade at chemoreceptors + Ach and α-adrenergic blockade;

 

SE - Sedation, dyskinesia, hypoT, glaucoma, additive CNS effects, ↓ seizure threshold

Term
Amitriptyline
Definition

TCA used to for chronic migraine prophylaxis;

Inhibits NE and Serotonin reuptake;

Anti-cholinergic;

 

SE - aggression, irritability, tachycardia, cycloplegia, xerostomia, constipation, urinary retention/BPH, endocrine dysfunction

Term
Divalproex
Definition

Anticonvulsant for chronic migraine prophylaxis;

Inhbits Na channels, ↓ GABA metabolism & reuptake [↑ GABA action]; Highly protein bound;

CYP2C9 substrate;

 

SE - TERATOGEN, N/V, pancreatitis, hepatotoxicity, sedation, weight gain.

Term
Valproic Acid
Definition

Anticonvulsant for chronic migraine prophylaxis;

Inhbits Na channels, ↓ GABA metabolism & reuptake [↑ GABA action]; Highly protein bound;

CYP2C9 substrate;

 

SE - TERATOGEN, N/V, pancreatitis, hepatotoxicity, sedation, weight gain.

Term
Propranolol
Definition

(Inderal)

For chronic migraine prophylaxis;

Prevents vasodilation, ↓ renin release and PG synth, ↑ O2 delivery;

EFFECTIVE FOR CHILDREN (the only drug proven effective for migraine prophylaxis in kids);

 

SE - lethargy, GI, exercise intolerance;

 

CI - asthma, AV block, sinus bradycardia, Diabetes

Term
Timolol
Definition

(Inderal)

For chronic migraine prophylaxis;

Prevents vasodilation, ↓ renin release and PG synth, ↑ O2 delivery;

 

SE - lethargy, GI, exercise intolerance;

 

CI - asthma, AV block, sinus bradycardia, Diabetes

Term
Topiramate
Definition

(Topamax)

Antiepileptic for chronic migraine prophylaxis;

Blocks Na channels, enhances GABA action, Inhibits Glutamate action;

 

Long duration but narrow Thereputic Index

 

SE: Parethesias, fatigue, nausea, narrow TI (toxicity risk)

Term
Botulinum toxin
Definition

(Botox)

For chronic migraine prophylaxis;

Inject symmetrically into glabellar frontalis and temporalis mm;

 

↓ incidence and severity of HA;

Limited SE;

High placebo rate

Term
Polymixin B Sulfate
Definition

Topical antibiotic;

Prevention of wound infection, early tx of infected dermatoses/wounds, prevention staph in nares;

Tx acne vulgaris, and used as an axillary deodorizer;

 

Avoid in open wounds;

SE: Neurotoxic and Nephrotoxic if systimically absorbed

Term
Gentamicin
Definition

Topical antibiotic,

(Also avail IV and IM, poor oral bioavail);

Used to prevent wound infection, in early tx of infected dermatoses/wounds, to prevent staph in nares, to tx acne vulgaris, and as an axillary deodorizer;

 

Limited in topical usage due to resistance fears;

 

SE - neuro-, nephro-, and oto-toxic* if absorbed

Term
Tetracycline
Definition

Topical antibiotic;

Used to prevent wound infection, in early tx of infected dermatoses/wounds, to prevent staph in nares, to tx acne vulgaris, and as an axillary deodorizer;

 

SE: Phototoxicity

CI - pregnancy, renal, hepatic dz, and in kids < 8 yo

Term
Clotrimazole
Definition

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Topical application is well tolorated.

 

CI: With Statins and Benzos

Term
Econazole
Definition

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Topical application is well tolorated.

 

CI: With Statins and Benzos

Term
Ketoconazole
Definition

Topical or Oral antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Topical application is well tolorated.

Oral SE of Antifungals: ↓ effects of anticoag drugs, oral contraceptives and cyclosporine immunosuppresants, ↑ effects of ethanol, cuases tachycardia, diaphoresis and flushing.

Inhibits CYP2C19, 3A4,5,7*; Inhibits testosterone synthesis.

CI: With Statins, Benzos, Cumadin/Warfarin, Oral contraceptives, cyclosporine, and ethanol.

Term
Miconazole
Definition

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Topical application is well tolorated.

 

CI: With Statins and Benzos

Term
Oxiconazole
Definition

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Topical application is well tolorated.

 

CI: With Statins and Benzos

Term
Sulconazole
Definition

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Topical application is well tolorated.

 

CI: With Statins and Benzos

Term
Ciclopirox
Definition

Non-azole, Topical antifungal agent

 

 

Term
Naftifine
Definition

Topical antifungal agent - allylamine;

Inhibits squalene monooxygenase to block sterol synthesis = compromised structural fungal integrity

Term
Terbinafine
Definition

Topical/oral antifungal agent - allylamine;
Inhibits squalene monooxygenase to block sterol synthesis to compromise structural integrity;

 

Inhbitor of CYP2D6 as oral agent,

 

CI - codeine, theophylline

Term
Butenafine
Definition

Topical antifungal agent - allylamine;

Inhibits squalene monooxygenase to block sterol synthesis to compromise structural integrity

Term
Tolnaftate
Definition
Topical antifungal agent - thiocarbamate;
Term
Nystatin
Definition

Topical antifungal agent - polyene;

Binds to ergosterol to compromise fungal cell wall integrity;

Term
Amphotercin B
Definition

Topical antifungal agent - polyene;

Binds to ergosterol to compromise fungal cell wall integrity;

Term
Griseofulvin
Definition

Oral antifungal agent;

Disrupts mitotic spindle/MT structure= metaphase arrest;

 

SE: leukopenia, proteinuria, ↓ anticoagulaiton effect of warfarin, ↓ contraceptive effects, ↓ cyclosporine serum levels, ↑ ethanol effects

 

Hepatic, Renal and Hematopoietic monitoring advised (due to leukopenia nd proteinuria effects)

Term
Fluconazole
Definition

Oral antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Oral SE of Antifungals: ↓ effects of anticoag drugs, oral contraceptives and cyclosporine immunosuppresants, ↑ effects of ethanol, cuases tachycardia, diaphoresis and flushing.

Inhibits CYP2C9;

CI: With Statins, Benzos, Cumadin/Warfarin, Oral contraceptives, cyclosporine, and ethanol.

Term
Itraconazole
Definition

Oral antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

 

Oral SE: ↓ effects of anticoag drugs, oral contraceptives and cyclosporine immunosuppresants, ↑ effects of ethanol, cuases tachycardia, diaphoresis and flushing.

 

Inhibits CYP3A4,5,7

CI: With Statins, Benzos, Cumadin/Warfarin, Oral contraceptives, cyclosporine, and ethanol.

Term
Clobetasol
Definition

VERY POTENT topical steroid;

↓ phospholipase A2 activity to ↓ inflammatory mediators; Immunomodulatory, anti-inflammatory, antipruritic, vasoconstrictive;

Acute control; Don't use on face, neck, groin;

 

SE - spread the infection, skin atrophy, glaucoma, hirsutism, acne, depigmentation, perioral dermatitis, Cushingoid Syndrome if systemically absorbed or used long-term.

Term
Budesonide
Definition

POTENT topical steroid;

↓ phospholipase A2 activity to ↓ inflammatory mediators; Immunomodulatory, anti-inflammatory, antipruritic, vasoconstrictive;

Acute control; Don't use on face, neck, groin;

 

SE - spread the infection, skin atrophy, glaucoma, hirsutism, acne, depigmentation, perioral dermatitis, Cushingoid Syndrome if systemically absorbed or used long-term.

Term
Betamethasone valerate
Definition

MODERATE strength topical steroid;

↓ phospholipase A2 activity to ↓ inflammatory mediators; Immunomodulatory, anti-inflammatory, antipruritic, vasoconstrictive;

Acute control; Don't use on face, neck, groin;

 

SE - spread the infection, skin atrophy, glaucoma, hirsutism, acne, depigmentation, perioral dermatitis, Cushingoid Syndrome if systemically absorbed or used long-term.

Term
Hydrocortisone
Definition

MILD topical steroid;

↓ phospholipase A2 activity to ↓ inflammatory mediators; Immunomodulatory, anti-inflammatory, antipruritic, vasoconstrictive;

Acute control; Don't use on face, neck, groin;

 

SE - spread the infection, skin atrophy, glaucoma, hirsutism, acne, depigmentation, perioral dermatitis, Cushingoid Syndrome if systemically absorbed or used long-term.

Term
Methylprednisolone
Definition

(Solu-Medrol)

PO, IV, IM steroid;

↓ phospholipase A2 activity to ↓ inflammatory mediators;

 

Tx resistant pyoderma gangrenosum, SLE, dermatomyositis

 

If given IV hypoT/HTN, hyperglycemia, hypo/hyperkalemia, anaphylaxism psychosis and CHF can result.

 

Withdrawl must be tapered.

Even with tapering, psoriasis pt can experience a pustular flare.

High dose withdrawl can produce arthralgias, myalgias and joint effusions.

Term
Tacrolimus
Definition

Topical/Oral

Blockade of Calcineurin blocks NFAT production whcih  ↓ inflammatory cytokines and ↓ T-, B-cell activation;

 

Tx atopic dermatitis;

 

Metabolized at CYP3A4 (metabolism blocked by grapefruit juice, Itra/ketoconazole, macrolide abx and others)

Term
Pimecrolimus
Definition

TOPICAL (only) Calcineurin blocker;

Blockade of Calcineurin blocks NFAT production which  ↓ inflammatory cytokines and ↓ T-, B-cell activation;

 

Tx atopic dermatitis;

 

SE - rxn w/ alcohol

Term
Imiquimod
Definition

TOPICAL immunosuppresant;

Unknown MoA (may effect DNA rep);

 

Tx external genital or perianal HPV warts;

Does not eliminate HPV and warts may reappear.

Term
Alefacept
Definition

IV/IM fusion protein - Immunosuppressant;

Modulates CD2 response, induces apoptosis of CD2+ cells;

 

Tx chronic plaque psoriasis;

 

SE - Lymphopenia*, secondary Basal/Squamous Cell carcinoma*,

production of neutralizing Abs (not clinically significant).

Term
Lindane
Definition

Tx scabies and pediculosis - 2nd line;

Topical liquid;

Absorbed into the parasites and their ova;

 

SE -BLACK BOX WARNING:seizures and death, CNS stimulant (blocks GABA's suppression)

Is slowly absorbed through the skin so the very young and very old/underweight are most succeptible to its toxicity.

Term
Crotaminton
Definition

Topical;

Unknown MoA;

 

Tx scabies and pediculosis;

Avoid inflamed or raw skin;

Term
Permethrin
Definition

(Nix)

Tx scabies and pediculosis - 1st line;

Topical;

Na channel disrupter = parasite death;

 

SE - none (low absorption + systemic inactivation)

Term
Malathion
Definition

Tx resistant scabies and pediculosis;

 

Remember: acetylcholinesterase inhibitor (insecticide);

 

SE - systemic ingestion=cholinergic effects (Miosis, sweating, chest tightness, wheezing, bradycardia, hypoT)

Term
Tretinoin
Definition

1ST Generation Retinoid - Oral;

Binda RAR (alpha, beta and gamma), 

↑ activity of RNA polymerase, ↓ epidermal cohesion, ↑ epidermal cell turnover;

 

Tx: inflammatory and hyperprolif dz, skin malignancies; Also used to enhance penetration of other agents (benzoyl peroxide, topical ABs);

 

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

Term
Isotretinoin
Definition

(Accutane)

1st Generation Retinoid - Oral;

Binda RAR (alpha, beta and gamma), 

↑ activity of RNA polymerase, ↓ epidermal cohesion, ↑ epidermal cell turnover;

 

Tx: inflammatory and hyperprolif dz, skin malignancies; Also used to enhance penetration of other agents (benzoyl peroxide, topical ABs);

 

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

Term
Acitretin
Definition

2ND Generation Retinoid - Oral;

Binds RAR (alpha, beta and gamma), 

↑ activity of RNA polymerase, ↓ epidermal cohesion, ↑ epidermal cell turnover;

 

Tx: inflammatory and hyperprolif dz, skin malignancies; Also used to enhance penetration of other agents (benzoyl peroxide, topical ABs);

 

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

Term
Adapalene
Definition

(Differin)

3RD Generation Retinoid - TOPICAL;

Binda RAR (alpha, beta and gamma), 

↑ activity of RNA polymerase, ↓ epidermal cohesion, ↑ epidermal cell turnover;

 

Tx: inflammatory and hyperprolif dz, skin malignancies; Also used to enhance penetration of other agents (benzoyl peroxide, topical ABs);

 

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

Term
Tazarotene
Definition

(Tazorac)

3RD Generation Retinoid - TOPICAL;

Binda RAR (alpha, beta and gamma), 

↑ activity of RNA polymerase, ↓ epidermal cohesion, ↑ epidermal cell turnover;

 

Tx: inflammatory and hyperprolif dz, skin malignancies; Also used to enhance penetration of other agents (benzoyl peroxide, topical ABs);

 

SE - dry skin, nose bleeds, conjunctivitis, alopecia, PHOTOSENSITIVITY, TERATOGEN

Term
Benzoyl peroxide
Definition

Topical;

Triggers oxidation of bacterial proteins, and is keratolytic (drying and desquamative);

Tx. - Propionibacterium acnes in sebaceous follicles and comedones;

 

SE - Xerosis, skin irritation, sting, +Hydroquinone= dark staining

Term
Azelaic acid
Definition

Keratolytic - topical;

Anti-microbial, anti-keratinizing, anti-inflammatory; Reversible inhibition of DNA polymerase, tyrosinase, and mitochondrial enzymes of the respiratory chain;

Causes mitochondrial swelling and accumulation of cytoplasmic lipid droplets.

Term
Salicylic acid
Definition

Keratolytic - topical;

Solubilizes cell surface proteins;

<6% is keratolytic and >6% is destructive.

 

SE - salicylism and death (even with topical drug, esp in kids, tx w/ dialysis), Contact/allergic dermatitis (urticaria, anaphylaxis, erythema multiforme)

Term
Propylene glycol
Definition

Keratolytic - topical;

 

SE - contact dermatitis

 

Often used in combination with 6% salicylic acid

Term
Minoxidil
Definition

(Rogaine)

Topical trichogenic agent , oral vasodilator;

 

Tx hair loss by unclear MoA;

 

SE - hypotension (if gets systemic); Avoid use at skin abrasions

Term
Finasteride
Definition

(Propecia)

Oral trichogenic;

Blocks DHT production;

 

Tx hair loss (in men only);

 

SE - sexual dysfunction;

 

CI w/ Saw palmetto

Term
Eflornithine
Definition

Topical Anti-trichogenic;

Unknown MoA, releated to ↓ levels ODC/polyamines;

 

Tx unwanted facial hair (face and chin only)

 

Ltd percutaneous absorption but avoid contact with eyes and mucous membranes.

 

Not a depilatory agent.

Term
Hydroquinone
Definition

[+Fluocinolone(corticosteroid) and + Tretinoin (retinoic acid) =Tri-Luma]

Bleaching agent;

Inhibits melanocyte production of DOPA, melanin formation;

 

Temporary tx of facial skin darkening 2nd to hormonal changes

Term
Methoxsalen
Definition

(UVADEX)

Oral/Topical Pigmentation/Darkening agent;

Stimulates melanocytes;

 

Tx vitiligo, psoriasis, cutaneous lymphoma, alopecia, inflamm dermatoses, eczema, lichen planus;

 

SE - +UV=erythema & ↑ melanin & cytotoxic effects + photosensitivity

Term
Drugs/classes that induce anaphylaxis (8)
Definition

Barbiturates

Etomidate (IV anesthetic)

Ester-type local anesthetics

Succinylcholine (NM blocker)

Meperidine (Opiate)

Morphine (Opiate)

Fentanyl (Opiate)

Antibiotics

Term
Clinical signs of Local Anesthetic toxicity
Definition

Minor Signs:

Ringing in the ears, metalic taste, numbness of the lips/tounge.

 

If these occur, Stop immedeatly.

 

Can lead to seizures if not addressed.

Term
Which pre-existing conditions (8) preclude the use of epinephrine?
Definition

Closed angle glaucoma (worsens the condition),

Heart failure (causes acute decompensation and arrhythmias),

Coronary dz (causes angina, MI),

HTN (angina, MI, stroke),

Rhythm disturbances (Heart failure, ventricular arrhythmias),

Cerebrovascular disorders (can cause stroke),

Hyperthyroidism (can cause tachycardia and HTN),

Diabetes (can cause Hyperglycemia)

Term
Which anesthetic has an "Induction Syndrome" occasionally associated with its use?
Definition

Propofol: Propofol Induction Syndrome

 

Iatrogenic Disease

Metabolic acidosis, rhabdomyolysis, arrhythmias, myocardial failure, renal failure, hepatomegly.

 

Risk Factors: CV incident, poor oxygen delivery, sepsis, high dose propofol tx.

 

Tx: Stop drug, stabilize circulation, correct acidosis, hemolysis (pt are usually not very responsive to ionotropes or cardiac pacing).

Term
Flumazenil
Definition

IV only

Specific benzodiazepine antagonist

Competitive inhibitor at the benzodiazepine binding site.

 

Used to reverse the effects of benzos in OD or in recovery.

Term
Remifentanil
Definition

A new Opiod;

[Sidenote: brush up on the other opiates as they are mentioned in the IV anesthetics lecture]

Very short-acting (rapid onset and peak effect in 1 min),

Half life: 10-20 mins,

Effects are non-cumulative and recovery is rapid;

Remember this means you're losing analgesia rapidly (keep in mind when dosing the pt, don't want pain to come back too fast).

Term
What happens when a pt is on N20 + Opiates?
Definition

Respiratory Depression!

Does not occur on N20 alone because it has balanced effects on respiration.

Addition of the opoioid decreases the responsiveness fo the carotid body and thereby depresses its response to rising PCO2.

Term
Malignant Hyperthermia
Definition

Pt: Typically young males who are genetically succeptible;

Triggers: Succinylcholine (depolarizing NM blocker, not for use in children), and/or all volitile anesthetic agents.

 

Causes ↑↑ in CO2, total body rigidity, tachycardia, tachypnea, and can lead to unexpected cardiac arrest.

Mechanism involves excess Ca2+ release from the SR.

 

Pt are hyperkalemic, acidodic (respiratory and metabolic), and have very high temperatures.

 

Tx: with Dantrolene (a muscle relaxation agent) + hyperventilate with O2, correct acidosis and hyperkalemia.

Avoid CCBs.

Term
What drugs are given 1-2 hours before surgery and what are the goals of this time period?
Definition

Benzodiazepine (ex: lorazepam, PO, sedation)

Opioid (ex: Morphine, IM, analgesia)

Scopolamine (a muscarinic antagonist, IM, amnesia/sedaiton)

Cimetidine and/or Metcolpramide (H2 antagonists, PO, inhibition of gastric acid release)

150 mL H2O (trigger stretch reflex causing natural gastric emptying)

Glycopyrrolate or Atropine (anticholinergics, IM, prophylaxis for the drying of secretions).

Term
What problems are there with using opioids for pain control in the peri-anesthetic period?
Definition

SE*

Orthostatic hypoT,

Epigastric distress (delay of GI transit and ↑ secretions),

N/V (both from epigastric distress and actions of opiates on central chemotrigger receptors, DA actions),

Respiratory depression/coma.

 

Term
Succnylcholine
Definition

A short-acting NM blocker;

Given following the IV bolus of sedative in Rapid Sequence Intubation (RSI);

 

SE and Tx of SE:

↑ ICP - give Lidocaine, Fentanyl, and/or Vercuronium;

Reactive airway  - give Lidocaine (blunts bronchospasm);

Bradycardia - Atropine in kids under 10 years;

Fassiculations - Vercuronium defassiculates

Term
Your pt is going in for surgery next week, when should you tell him/her to stop current medications?
Definition

NEVER!

Because of significant withdrawl and adverse effects of stopping longstanding medications, pt should always be advised to stay on these medications and the anesthesia should be adjusted accordingly.

Term
What agents/classes of drugs have been associated with anaphalactic reactions?
Definition

Induction agents: Drugs solubilized in cremophor, barbituates, etomidate.

 

Local anesthetics: benzoic ester type

 

Muscle Relaxants: Succinylcholine, gallamine, pancuronium, tubocuarine, metocurine, atacurium.

 

Narcotics: Meperidine, Morphine, Fentanyl

 

Abx, bone cement, radiocontrast dye, additives, blood products, colloid volume expanders.

Term
A pt in for surgery begins to have an anaphylactic reaction, what do you do?
Definition

1. Discontinue the offending agent and stop anesthesia

2. Give O2 and Epinephrine (CV support)

3. Expand the intravascular volume using Isotonic Crystalloid.

 

4. Treat effects secondarily

Anti-histamines, catecholamines, methyxanthines (when pt has persistant bronchospasm), corticosteroids, sodium bicarbonate (if the pt has acidosis).

Term

Describe the role and location of the following receptors:

5-HT1B

5-HT1D

Definition

5-HT1B receptors are located directly on the vasculature and mediate vasoconstriction (a desired effect in the tx of migraines, hence the use of serotonin agonists).

 

5-HT1D receptors are located on the nerve terminal and act to attenulate cacium influx and thereby modulate the release of infalmmatory mediators (CGRP and SP)

Term
Caffeine
Definition

Used in the acute tx of migraines;

A Cerebral Vasoconstrictor*;

 

Particularily useful if caffeine withdrawly (which involves vasodilation) is invovled in the pathogenesis of the HA;

 

Potential CV (proarrhythmic) effects.

Term
What is allodynia and what drugs are useful in its management?
Definition

Allodynia is pain due to a stimulus that does not normally produce pain.

 

Is present in 80% of all migraines.

 

Triptans are particularily useful in tx allodynia.

Term
Which drugs from this assessment have CYP3A4 interactions and what medications should they not be given with?
Definition

Opiates,

Ergots,

 

AVOID:

SSRI, HIV drugs, and Azole antifungals

Term
What drugs have High/Moderate/Low risk of development of Analgesic Overuse Syndrome?
Definition

High Risk:

Asprin/Acetaminophen/Caffiene,

Drugs containing Butalbital,

Opiods.

 

Moderate Risk: Triptans and Short acting NSAIDs.

 

Low Risk: Long acting NSAIDs, Tramadol (weak opoid with monamine reuptake blockade), and Dihydroergotamine (DHE).

Term
What are some possible causes of and ways to treat Analgesic Overuse Syndrome?
Definition

Possible Causes: Trigeminovascular sensitization, drug-induced ↓ of 5-HT levles/5HT receptor upregulation, Cellular adaptation, free radical damage to the periaquueductal grey tissue.

 

Treatment: A 3 faceted approach;

Transition or Bridging program involves control with Ergotamine and prophylaxis with Propanolol + tx with Tizanidine (an antispasmodic alpha-2 agonist) + a long-acting NSAID.

Use of drugs with low potential to trigger the syndrome.

Biofeedback, Prophylaxis, Cognitive behavior therapy, and relaxation training also used.

Term
Contraindications of Azole Antifungals
Definition

Statins

(atorvastatin, cerviastatin, locastatin, simvastatin)

↑ risk of myopathy, rhabdomyolysis, and acute renal failure.

 

Benzodiazepines (Midazolam and triazolam)

Also reduced clearance of alprazolam and estazolam.

Term
Cyclosporine
Definition

Oral;

Immunosuppressant; Blockade of Calcineurin blocks NFAT production whcih  ↓ inflammatory cytokines and ↓ T-, B-cell activation;

Does not affect suppressor T cells or Ab-mediated immunity.

 

Tx: Severe plaque-type psoriasis, transplant immunosuppressant.

 

Classic SE: Nephrotoxicity

Renal vasoconstriction, ↑ creatinine, arterial bp and serum K+ [This effect is more typical in the doses given to transplant pt than those used to tx psoriasis.]

Term
Topical use of Antivirals and Antihistamines
Definition

Drugs listed in these categories in our notes are not on the drug list.

 

Both classes can be used orally and topically

 

Topical Antivirals: often used to tx herpes simplex!

 

Topical Antihistamines: used to tx acute and chronic urticaria and allergic rxns.

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