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.

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

Liquid Inhalation Anesthetic;

2nd (of 3) agent of choice;

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

Liquid Inhalation Anesthetic;

'1st' agent of choice;

SE - areflexia, irritant, muscle relaxation, hypoventilation

Liquid Inhalation Anesthetic;

'1st' agent of choice - newer;

Accumulates and equilibrates quickly,

PLUS rapid recovery;

SE - areflexia, irritant, hypoventilation

Liquid Inhalation Anesthetic;

'1st' agent of choice - newer;

Accumulates and equilibrates quickly,

PLUS rapid recovery;

SE - areflexia, hypovent, CV depression

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

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

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

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).

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

(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)

(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)

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)

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.

Local anesthetic - Amide (hepatic metabolism);

Injectable (no topical effects);

Blocks Na channels, ↑ refractory period;

Slow onset, intermediate duration;

Local anesthetic - Amide (hepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

Rapid onset, intermediate duration; 

↓ acute tox;

SE - Methemoglobinemia (Ferric Hb, cyanosis)

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!)

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.

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).

Local anesthetic - Ester (extrahepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

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

Minimal fetal exposure

Local anesthetic - Ester (extrahepatic metabolism);

Injectable;

Blocks Na channels, ↑ refractory period;

Slow onset, long action;

HIGH POTENCY; Potentially very toxic

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

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

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

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);

TOPICAL local anesthetic;

Blocks Na channels, ↑ refractory period;

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

TOPICAL local anesthetic;

Blocks Na channels, ↑ refractory period;

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

Common ER prep;

Topical local anesthetic mixture;

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

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.

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.

(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

H1 antagonist;

  POand IM;

SEDATIVE,

anticholinergic, antiemetic

(Benadryl)

H1 anti-histamine (CNS actions);

PO and IM;

SEDATIVE, ANTICHOLINERGIC, antiemetic

(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

(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

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.

Non-particulate Antacid;

Na- and K-citrate + citric acid;

Neutralizes existing contents of stomach

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.

(Zofran)

Serotonin (5-HT3) receptor antagonist;

Anti-emetic; Expensive, reserved for severe cases

Antibiotic,

Prophalyxis of infection;

Ancillary drug to anesthesia;

Tx STAPH AND STREP

Antibiotic, prophalyxis of infection;

Ancillary drug to anesthesia;

Tx: infection with BOWEL ANEROBES

Antibiotic, prophalyxis of infection;

Ancillary drug to anesthesia;

Tx infection with BOWEL ANEROBES

Antibiotic, prophalyxis of infection;

Ancillary drug to anesthesia;

Reserve use for when MRSA is suspected,

Routine use is discouraged.

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

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

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)

Rapid sequence intubation-

Decreases fasciculations and mitigates ICP response to Succinylcholine

Rapid Sequence Intubation;

↓ sympathetic response to procedure;

Indicated if ↑ ICP, hemorrhage, CV dz

Ancillary: post-op CV support;

Tx hypoT;

Has a beta effect on heart and maintains renal perfusion

(AK-Dilate)

Ephedrine can also be used, same indications/SE*

Pressor/sympathomimetic: alpha-agonist;

Ancillary: post-op CV support; 

Tx hypoT;

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)

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.

Ancillary: tx post-op Anaphylaxis;

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

Ancillary: tx post-op Anaphylaxis;

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

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.

(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

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.

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

NSAIDs

Opiates

Triptans

Ergot's

(Anti-emetics)

Triptan

1st line tx for mod/severe acute migraine;

5-HT_{1B & 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).

Triptan

1st line tx for mod/severe acute migraine;

5-HT_{1B & 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).

(Imitrex) Triptan

1st line tx for mod/severe acute migraine;

5-HT_{1B & 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).

Triptan

1st line tx for mod/severe acute migraine;

5-HT_{1B & 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).

Ergot for acute SEVERE migraine tx;

Agonist on 5-HT_1&2, α_1&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)

Ergot for acute SEVERE migraine tx;

Agonist on 5-HT_1&2, α_1&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)

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

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

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

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.

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.

(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

(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

(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)

(Botox)

For chronic migraine prophylaxis;

Inject symmetrically into glabellar frontalis and temporalis mm;

↓ incidence and severity of HA;

Limited SE;

High placebo rate

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

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

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

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

Topical application is well tolorated.

CI: With Statins and Benzos

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

Topical application is well tolorated.

CI: With Statins and Benzos

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.

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

Topical application is well tolorated.

CI: With Statins and Benzos

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

Topical application is well tolorated.

CI: With Statins and Benzos

Topical antifungal agent - azole derivative;

↓ production of ergosterol compromising fungal cell wall integrity;

Topical application is well tolorated.

CI: With Statins and Benzos

Non-azole, Topical antifungal agent

Topical antifungal agent - allylamine;

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

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

Topical antifungal agent - allylamine;

Inhibits squalene monooxygenase to block sterol synthesis to compromise structural integrity

Topical antifungal agent - polyene;

Binds to ergosterol to compromise fungal cell wall integrity;

Topical antifungal agent - polyene;

Binds to ergosterol to compromise fungal cell wall integrity;

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)

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.

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.

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.

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.

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.

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.

(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.

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)

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

TOPICAL immunosuppresant;

Unknown MoA (may effect DNA rep);

Tx external genital or perianal HPV warts;

Does not eliminate HPV and warts may reappear.

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).

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.

Topical;

Unknown MoA;

Tx scabies and pediculosis;

Avoid inflamed or raw skin;

(Nix)

Tx scabies and pediculosis - 1st line;

Topical;

Na channel disrupter = parasite death;

SE - none (low absorption + systemic inactivation)

Tx resistant scabies and pediculosis;

Remember: acetylcholinesterase inhibitor (insecticide);

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

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

(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

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

(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

(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

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

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.

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)

Keratolytic - topical;

SE - contact dermatitis

Often used in combination with 6% salicylic acid

(Rogaine)

Topical trichogenic agent , oral vasodilator;

Tx hair loss by unclear MoA;

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

(Propecia)

Oral trichogenic;

Blocks DHT production;

Tx hair loss (in men only);

SE - sexual dysfunction;

CI w/ Saw palmetto

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.

[+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

(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

Barbiturates

Etomidate (IV anesthetic)

Ester-type local anesthetics

Succinylcholine (NM blocker)

Meperidine (Opiate)

Morphine (Opiate)

Fentanyl (Opiate)

Antibiotics

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.

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)

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).

IV only

Specific benzodiazepine antagonist

Competitive inhibitor at the benzodiazepine binding site.

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

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).

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.

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.

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).

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.

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

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.

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.

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).

Describe the role and location of the following receptors:

5-HT_1B

5-HT_1D

5-HT_1B 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-HT_1D receptors are located on the nerve terminal and act to attenulate cacium influx and thereby modulate the release of infalmmatory mediators (CGRP and SP)

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.

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.

Opiates,

Ergots,

AVOID:

SSRI, HIV drugs, and Azole antifungals

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).

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.

Statins

(atorvastatin, cerviastatin, locastatin, simvastatin)

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

Benzodiazepines (Midazolam and triazolam)

Also reduced clearance of alprazolam and estazolam.

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.]

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.