Anti-coagulant;

Neg charged glycoprotein, binds to exosite 2 on ATIII, enhancing its activity = inactivation of thrombin + factors IX, X, XI, XII;

Admin SQ or IV;

Rapid onset of axn* Variable t_1/2;

Non specific = binding to other plasma proteins (incl PF4)- monitor PTT;

Works only for soluble thrombin;

Indications: ACS/MI, acutely in coronary angioplasty/Afib/DVT/PE;

SE: HIT (formation of an immunogenic heparin-PF4 complex at 5-10 days resulting in clot formation), bleeding risk, osteoporosis;

Antidote: Protamine Sulfate (+ charge, chelates)

Low MW Heparin;

Admin SQ;

Smaller active components, longer t_1/2;

Increased anti-Xa axn*, reduced plasma protein binding, and anti-platelet action;

No need to monitor*;

Indications: DVT prophylaxis;

SE: Less potential for HIT (at 5-10 days) - still possible

Low MW Heparin;

Admin SQ;

Smaller active components, longer t_1/2;

Increased anti-Xa axn*, reduced plasma protein binding, and anti-platelet action;

No need to monitor*;

Indications: DVT prophylaxis;

SE: Less potential for HIT (at 5-10 days) - still possible

Low MW Heparin;

Admin SQ;

Smaller active components, longer t_1/2;

Increased anti-Xa axn*, reduced plasma protein binding, and anti-platelet action;

No need to monitor*;

Indications: DVT prophylaxis;

SE: Less potential for HIT (at 5-10 days) - still possible

Low MW Heparin;

Admin SQ;

Smaller active components, longer t_1/2;

Increased anti-Xa axn*, reduced plasma protein binding, and anti-platelet action;

No need to monitor*;

Indications: DVT prophylaxis;

SE: Less potential for HIT (at 5-10 days) - still possible

Low MW Heparin;

Admin SQ;

Smaller active components, longer t_1/2;

Increased anti-Xa axn*, reduced plasma protein binding, and anti-platelet action;

No need to monitor*;

Indications: DVT prophylaxis;

SE: Less potential for HIT (at 5-10 days) - still possible

Low MW Heparin;

Admin SQ;

Smaller active components, longer t_1/2;

Increased anti-Xa axn*, reduced plasma protein binding, and anti-platelet action;

No need to monitor*;

Indications: DVT prophylaxis;

SE: Less potential for HIT (at 5-10 days) - still possible

Low MW Heparin;

Admin SQ;

Smaller active components, longer t_1/2;

Increased anti-Xa axn*, reduced plasma protein binding, and anti-platelet action;

No need to monitor*;

Indications: DVT prophylaxis;

SE: Less potential for HIT (at 5-10 days) - still possible

Direct Thrombin Inhibitor (from leech saliva);

Irreversibly binds the thrombin active site and exosite 1;

Acts on soluble and clot-bound;

No immune-med thrombocytopenia (no HIT);

Tx: Heparin Induced Thrombocytopenia (HIT);

SE: (less) hemorrhage;

CI - renal failure

Recombinant Hiruden;

Direct Thrombin Inhibitor (from leech saliva);

Irreversibly binds thrombin active site and exosite 1;

Acts on soluble and clot-bound;

No immune-med thrombocytopenia (no HIT);

Tx: Heparin Induced Thrombocytopenia (HIT);

SE: (less) hemorrhage;

CI - renal failure

Vitamin K Antagonist;

Competes w/ Vitamin K epoxide reductase - ↓ vitamin K synthesis blocking activation of factors II, VII, IX, X - ↓ thrombin formation;

Slow onset (36-72 hrs), long duration;

Monitor PT*;

Tx: DVT, PE, Afib, Rheumatic heart dz (DOC for 1st 3);

SE: Skin necrosis (think Protein C def), hemorrhage, transient pro-coagulant (inhibits Protein C synthesis too), drug interactions (incl. EtOH*);

CI: liver disease

Vitamin K Antagonist;

Competes w/ Vitamin K epoxide reductase (VKER) - ↓ vitamin K synthesis blocking activation of factors II, VII, IX, X - ↓ thrombin formation;

Slow onset (36-72 hrs), long duration;

Monitor PT*;

Tx: DVT, PE, Afib, Rheumatic heart dz (DOC for 1st 3);

SE: Skin necrosis (think Protein C def), hemorrhage, transient pro-coagulant (inhibits Protein C synthesis too), drug interactions (incl. EtOH*);

CI: liver disease;

Metabolic variations possible at VKER and CYP2C9*

Vitamin K Antagonist;

Competes w/ Vitamin K epoxide reductase - ↓ vitamin K synthesis blocking activation of factors II, VII, IX, X - ↓ thrombin formation;

Acetylsailycilic acid;

Non-selective COX1/2 irreversible inhibitor;

Analgesic, antipyretic, anti-plateletA (dt acetylation);

COX1 inh - no PLT TXA2 - ↓ PLT aggregation. COX2 inh - no endothelial PGI2 - ↑ aggregation;

Tx: Stable CHD, ACS/MI, coronary angioplasty, TIA/stroke, Afib, DVT/PE;

SE: GI bleeding, hemorrhagic stroke, asthma (dt ↑ LTs);

CI: Coumarin (Warfarin, dt ↑ bleeding risk), PUD, asprin hypersensitivity/asthma;

Max dose <4g/day

(Ibuprofen, Naproxen, etc...);

Reversible non-selective COX1/2 inhibitors - anti-platelet;

COX1 inhibition - no TXA2 - ↓ aggregation;

COX2 inhibition - no PGI2 - ↑ aggregation;

Reversibility means that these agents have much worse anti-platelet action than Asprin (do not reduce CHD);

Should not be taken at the same time as Asprin (blocks the effects of Asprin preventing its antiplatelet action which may actually ↑ risk of CVD)

Selective COX2 Inhibitor;

Specifically an anti-inflammatory agent (tx RA and other chronic inflammatory conditions);

No antiplatlet effects;

No PGI2 = ↑ platelet aggregation = ↑ risk of CVD/CHD;

SE: ↑ CHD/CVD dt unoppsed TXA2 action (via uninhibited COX1 which = hyperactivation of platelets and clot formation!), and HTN (blocking COX2 = blockage of prostacyclin, a vasodilator = HTN)

PDE Inhibitor - anti-platelet;

↑ cAMP = inhibits prostacyclin-mediated  PLT aggregation and ↑ adenylate cyclase (↓ adenosine);

Vasodilator;

Tx: Not used alone - with Aspirin for anti-platelet effects (avail in a combo pill, synergy in anti-PLT axn), or with warfarin to ↓ thromboembolic events in pts with prosthetic valves;

Also admin IV to induce coronary steal in cardiac studies;

SE: (all are dt the vasodilitory effects of the drug) HA, dizziness, GI, coronary steal* (diversion of blood away from the heart with in a pt with artery narrowing put on a vasodilator)

Specific, reversible inhibitor of PDE IIIB - anti-platelet;

Vasodilator;

Not a primary antiplatelet drug;

Tx: Intermittent claudication (leg pain) in peripheral arterial dz;

Anti-PLT action is not a primary indication, rather an added benefit of this drug;

PGI;

Direct Adenylate Cyclase activator (via G-protein-coupled receptor) - anti-platelet;

↑ cAMP which inhibits platelet aggregation

Indirect Adenylate Cyclase activator - anti-platelet;

↑ cAMP to inhibit platelet aggregation

Plavix;

ADP Inhibitor - anti-platelet - Thienopyridine;

Prodrug* - activated by CYP2C19 (pt on omeprazole and those with genetic lack of CYP2C19 req ↑ dose);

Prevents ADP-mediated externalization of the GPIIb/IIIa receptor - no platelet aggregation! Effective;

Tx: CHD in higher risk pts - unstable angina or NSTEMI with asprin admin first and indefinitely (not recommended for use in stable CHD*), Prophylaxis for MI, stroke (with Asprin);

SE: Bleeding!;

CI: Recent surgery (must dc 5+ days before undergoing CABG or other surgery;

DirectGPIIb/IIIa Receptor Blocker - anti-platelet;

Synthetic polypeptide - IV admin;

Prevents aggregation of PLT by preventing binding of fibrinogen or vWF via GPIIb/IIIa block;

Tx: non-Qwave MI, given acutely, prior to cardiac cath or angioplasty to prevent in-stent thrombosis/stenosis;

Acute infusions are typically with Asprin and Heparin prior to/during the procedure - shown to reduce CHD/MI death during these procedures.

GP IIb/IIIa Receptor Blocker - anti-platelet;

Monoclonal Ab (Fab fragement) that targets the receptor;

IV admin;

Tx: Given before/during cardiac cath and angioplasty;

Helps restore blood flow in failed rescue angioplastys*

1st Gen Fibrinolytic/Thrombolytic;

Forms activator complex with plasminogen;

Non-specific activation of circulating and fibrin-bound plasminogen;

Tx: MI, PE, DVT, thrombotic stroke;

SE: (dt non-spec axn & Strep immunogenicity) Systemic lytic state, intracranial hemorrhage, immune response (hypoT, bronchospasm, angioedema, serum sickness);

CI: Age >75 yrs, recent surgery, HTN, pericarditis (can lead to hemopericardium), prior use/recent strep infx (one time use deal);

1st Gen Thrombolytic;

From cultures of human fetal kidney cells - nonantigenic;

Non-specific Serine protease that cleaves plasminogen to plasmin;

Tx: Acute, massive, or hemodynamically unstable PE;

SE: Systemic lytic state (dt non-specific axn), intracranial hemorrhage;

CI: Age > 75 yrs, surgery, HTN, pericarditis;

2nd Gen Thrombolytic;

Recombinant version of a naturally occuring (produced by vascular endothelial cells) serine protease;

Forms tertiary complex* w/ fibrin and plasminogen; Specific action for fibrin and localization to the clot;

IV (front-loaded) infusion - peptide composition requires a continuous IV infusion*;

Tx: MI, PE, or ischemic stroke (if within 3 hrs and there is no evidence of hemorrhage);

Marginally ↑ patency rates/↓ mortaility over 1st gen;

3rd Gen Thrombolytic;

r-PA - "small t-PA" (kringle + protease);

Long t1/2, does not require continuous infusion;

Admin IV bolus;

Efficacy similar to streptokinase;

SE: ↑ incidence hemorrhagic stroke;

H2 antagonist - PUD, GERD;

Competitively inhibits H2 receptors in stomach, ↓ acid secretion;

CYP2C19 inhibitor;

Least potent in class, short half life;

Use <2 weeks, not for use in kids <12 y.o.;

SE: HA, dizzy, GI

H2 antagonist - PUD, GERD;

Competitively inhibits H2 receptors in stomach, ↓ gastric acid secretion;

Use <2 weeks, not in kids <12 y.o.;

Most potent and longest 1/2 life in class*;

SE: HA, dizzy, GI

H2 antagonist - PUD, GERD;

Competitively inhibits H2 receptors in stomach, ↓ gastric acid secretion;

Use <2 weeks, not in kids <12 y.o.;

SE: HA, dizzy, GI

H2 antagonist - PUD, GERD;

Competitively inhibits H2 receptors in stomach, ↓ gastric acid secretion;

Use <2 weeks, not in kids <12 y.o.;

SE: HA, dizzy, GI

Milk of Magnesia - Antacid;

Weak bases neutralize HCl, prevents pepsin activation;

Tx: reflux, adjunct w/ H2 block or PPIs in PUD;

SE: ↓ drug absorption, constipation or diarrhea, electrolyte imbalance, kidney stones*;

Caution: pt with bone dz or in Renal Failure;

Lots of Drug-Drug Interactions: Chelates tetracyclines and quinolones altering their absorption, also increases urine pH reducing the solubility of the fluroquinolones in the urine leading to stone formation*

Antacid;

Weak base neutralizes HCl, prevents pepsin activation;

Tx: Reflux, adjunct w/ H2 block or PPIs in PUD;

SE: ↓ drug absorption, (less) constipation or diarrhea, electrolyte imbalance, kidney stones

Antacid;

Weak base, neutralizes HCl, prevents pepsin activation;

Tx: Gas, PUD, acid (↑ pH);

SE: ↓ drug absorption, constipation or diarrhea, electrolyte imbalance, kidney stones

[Kaopectate]

Anti-Diarrheal and Cytoprotective agent;

Absorbs hermful bacteria/viruses/toxins, ↑ secretion of mucous and HCO₃, inhibits Pepsin release, chelates w/ proteins at base of ulcer forming protective barrier, inhibits H. pylori growth;

Tx: Travellers diarrhea and H. Pylori infection;

SE: significant drug interactions*;

CI: Fever, blood or mucous in stool (infection)

Opiate Anti-diarrheal;

↓ secretions, ↑ muscle tone (antispasmodic*) including sphincters (↓ urgency @external anal sph), ↓ motility, ↑ GI contact time;

Binds calmodulin;

Tx: Diarrhea;

CI: fever, blood or mucous in stool

1st Gen Antihistamine;

Sedative, anti-emetic, GI cramps, anticholinergic;

Tx: Allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);

SE: Sedation, dystonia, nasal congestion, hallucinations, inhibited diaphoresis*, anuresis, arrhythmia;

CI: Asthma, glaucoma

1st Gen Antihistamine;

Sedative, anti-emetic, GI cramps, anticholinergic;

Tx: Allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);

SE: Sedation, dystonia, nasal congestion, hallucinations (abuse), inhibited diaphoresis*, anuresis, arrhythmia;

CI: Asthma, glaucoma

1st Gen Antihistamine;

Sedative, anti-emetic, GI cramps, anticholinergic;

Tx: Allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);

SE: Sedation, dystonia, nasal congestion, hallucinations, inhibited diaphoresis*, anuresis, arrhythmia;

CI: Asthma, glaucoma

2nd Gen antihistamine;

Appetite stimulation, some sedation;

Longer duration of action, 'non-sedating', no anticholinergic effects - SAFE for asthmatics;

Tx: Allergy, hayfever, rhintis, urticaria, insect bites, contact flora;

SE: Mild congnitive disturance, some appetite stimulation

1st Gen antihistamine;

Sedative, anti-emetic, GI cramps, anticholinergic;

Tx: Allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);

SE: Highly Sedative, dystonia, nasal congestion, hallucinations (abuse), inh diaphoresis, anuresis, arrhythmia, mydriasis;

CI: asthma, glaucoma

2nd Gen antihistamine;

Appetite stimulation, some sedation;

Longer duration of action, 'non-sedating', no anticholinergic effects - SAFE for asthmatics;

Tx: Allergy, hayfever, rhintis, urticaria, insect bites, contact flora;

SE: Mild congnitive disturance, some appetite stimulation

Weak Inhibitor of COX-1/2, stronger Brain COX (3) inhibitor;

Analgesic and antipyretic;

Limited/no effect on platelets;

NOT useful for anti-inflammatory;

Tx: Antipyretic/analgesic for patients taking warfarin or heparin, also prefered in pregnant women/children* (avoid Asprin and NSAIDS in these groups);

SE: Hepatotoxicity*, stroke, MI;

CI: Excessive EtOH, >60y.o.(caution);

Max dose <4g/day

NSAID - reversible, non-selective COX inhibitor;

Anti-platelet (prolonged bleeding), anti-inflammatory, antipyretic, and analgesic actions;

Tx: RA (3200mg), pain (400mg/6hrs);

SE: HTN*, GI irritation (less than others), stroke, MI;

CI: Pregnancy, excessive EtOH intake, >60y.o. (caution), renal failure, peptic ulcer dz;

Max dose <4g/day

NSAID - reversible COX inhibitor;

Anti-platelet (prolonged bleeding), anti-inflammatory, antipyretic, and analgesic actions;

Long half-life - 14hrs, so 2xday dosing*;

SE: GI irritation, stroke, MI;

CI: High EtOH, >60y.o.(caution), renal failure, PUD;

Max dose <4g/day

Antitussive - Requires a Perscription*

Mu Opiate Receptor agonist (morphine-like);

Low affinity, 10% converted to morphine;

Oral or parenteral admin;

Resistance in 10% caucasians;

Tx: Mild pain, Cough suppressant (central suppression of the cough center in the brainstem medulla);

Lacks controlled studies, deaths reported in kids;

Biotransformation to Morphine is via CYP2D6 and ultra rapid metabolsers can produce life-threatening resp depression and issues for breast-feeding neonates*

Antitussive - cough suppression - in>125 OTC products;

Opiate deriv:non-narcotic, axn on many receptor types (not exclusively opoid receptors);

At normal doses no sedative, analgesic or addictive fx*;

Met at CYP2D6 (deficient in some = acute toxicity); 

SE: Hallucinogen, dry mouth, tachycardia, disorientation, depersonalization, somnolence, addiction (at high doses/frequent use);

Abuse: Produces a Phencyclidine (PCP) like effects when abused (out of body, high, dissociative anesthesia, highly addictive) - combo products are now formulated with toxicity if over-used to limit abuse.

Only FDA-approved OTC Expectorant;

Often combined w/ antihistamines, antitussives;

Tx: Productive cough w/congestion;

SE: (@high doses) N/V dizziness, HA, rash

Alpha Agonist and topical Decongestant (Afrin);

Use for <3 days  to avoid rebound congestion (rhinitis medicamentosa);

Long acting!;

Direct and indirect sympathomimetic axn - ↑ presynaptic NE release;

SE: HTN, Rhinitis medicamentosa, tachy/arrhythmia;

Interactions: Beta blockers, Digoxin, MAOIs;

CI: thyroid dz*, DM, BPH/urinary retention, closed angle glaucoma

Nasal Decongestant;

Alpha 1 receptor agonist;

'Topical' or Oral Admin;

Use for <3 days - rebound congestion;

SE: HTN, Rhinitis medicamentosa (topical), tachycardia/arrhythmia;

CI: thyroid dz, DM, BPH, glaucoma

Decongestant;

'Topical' Admin;

Use for <3 days to avoid rebound congestion;

Long acting!;

Direct and indirect sympathomimetic axn - ↑ presynaptic NE release;

SE: HTN*, Rhinitis medicamentosa, tachy/arrhythmia;

CI: thyroid dz, DM, BPH, glaucoma

Decongestant and allergy;

Oral admin;

Methamphetamine precursor - regulated sales;

Direct and indirect sympathomimetic axn - ↑ presynaptic NE release;

SE: HTN, glaucoma, vasospasm, arrhythmia, stroke, seizure, hallucinations, HA, insomnia, tremor;

Interaxns: BB, digoxin, MAOIs = tachy/arrhythmia;

CI: thyroid dz, DM, BPH, glaucoma

 [Unisom]

Antihistamine - Sleep aid;

Use <2 weeks;

SE: Hallucinations (abuse), euphoria, anticholinergic efx, mydriasis

Citrucel;

Bulk-Forming Laxative - safest;

Cause the stool to be bulkier and to retain more water, as well as forming an gel, making it easier to move it along;

Take with water;

Bulk-producing agents are the most gental laxatives and can be taken just for maintaining regular bowel movements.

Hyperosmotic Laxative;

Detergent action;

Local irritation or distention from ↑ volume;

Laxative;

Detergent action;

Local irritation or distention from increased volume;

Smoking cessation;

Best efficacy in combination with cessation programs and pharmacologic aids;

Must retain in mouth for 20-30 minutes;

CI: oral lesions/dental work, active smoking

Smoking cessation;

Best efficacy in combination with cessation programs;

Smoking cessation;

Patch, variable time to peak plasma concentration;

Well tolerated;

Best efficacy in combination with cessation programs;

SE: sleep disturbance, skin irritation;

CI: active smoking

Anti-Spasticity Agent and Skeletal Muscle Relaxant;

Acts as a GABA_B agonist in the SC (inhibitory signals or reducing excitatory pathways) and inhibition of substance P action (pain relief);

Oral or Intrathecal (higher lvls reached w oral) admin;

Tx: Multiple sclerosis, muscle spasm, spasticity, and SC trauma;

SE: Drowsiness, asthenia, confusion, dizziness, fatigue, headache, rebound neural activity (seizures, hallucinations, psych disturbances) if not tapered*;

Interactions: Additive CNS depression w/ other CNS depressants and MAOIs, HypoT w/ MAOIs and other antihypertensives, dose adj req w/ antidiabetic agents- Baclofen ↑ blood glucose;

CI: Impaired renal function (drug accumulation and severe side effects)

Anti-Spasticity Agent and Skeletal Muscle Relaxant;

Pre-synaptic α2 receptor agonist = ↓ activation of polysynaptic SC motor neurons and ↓ muscle tone but not strength (anti-HTN axns are very weak);

Short t_1/2, dose adjustment req w ↑ age and ↓ CrCl;

Tx: Multiple sclerosis, spasticity, and SC trauma;

SE: Asthenia, xerostomia, dizziness, sedation, hypoT;

Interactions: Additive CNS depression, ↑ toxicity with Rofecoxib (NSAID), ↑ drug levels with fluvoxamine;

CI: With clonidine, methyldopa, guanfacine, or guanabenz (severe hypoT)

Anti-Spasticity Agent, Skeletal Muscle Relaxant, and Antidote;

Ryanodine Receptor (on the sarcoplasmic reticulum of muscle cells) antagonist. Reduces musclar response to direct stimulation = mild weakness w improved tone*;

Oral or IV admin;

Tx: Multiple sclerosis, spasticity, malignant hyperthermia, neruoleptic malignatn syndrome (hyperthermia, musclar rigidity, and ↑ CK);

SE: Muscle weakness (drooling, enuresis, myalgias), Pulmonary edema/seizures/pericarditis (rare), injection site phelbitis.

Hepatotoxicity with Estrogens* (Check LFTs), crosses the placenta (floppy baby if used in C section);

Interactions:Additive CNS depression, IV dantroline +CCB (tx malignant hyperthermia) may produce Vfib and CV collapse;

Older Anti-Spasticity Agent - does not actually do this;

Still on the market as an anti-malarial drug but can no longer be advertised as a drug to tx nocturnal leg cramps (esp since the side effects are so severe);

Skeletal Muscle Relaxant;

Gneralized sedation (no direct effects on neuronal conduction, neuromuscular transmission, or muscular excitability);

Oral admin;

Tx: Muscle spasm;

SE: Drowsiness, dizziness, agitation, insomnia, vertigo, ataxia, temp vision loss, mydriasis, orthostatic hypoT;

Interactions: at CYPs (plasma levels ↓ with inducing agents, rifampin/carbamazepine, or ↑ with blockers, ketoconazole/fluoxetine), additive CNS depression

Skeletal Muscle Relaxant;

Unknown MoA but probably generalized sedative action and alteration of pain perception;

Oral admin;

Tx: Muscle spasm;

SE: Hepatotoxicity (monitor LFTs), drowsiness/sedation, agitation, lightheadedness, paradoxical stimulation;

Interactions: Additive CNS depression (incl with EtOH), potential isoniazid and disulfram interactions via CYP;

Skeletal Muscle Relaxant;

Commonly used - related to TCAs;

Cnetral axn, possibly brain stem. Undergoes extensive interohepatic recirculation and hepatic elim (adjust age in the elderly and pt with hepatic impairment);

Oral admin;

Tx: muscle spasm and off-label for fibromyalgia;

SE: Significant anticholinergic action (drowsiness, xerostomia, dizziess, blurred vision), confusion and cardiac effects in the elderly;

Severe GI problems with combined use of other anticholinergics and/or TCAs - Paralytic ileus*;

Lots of Interactions: Addive CNS depression with other depressants and anticholinergic axn with anticholinergic and 1st gen antihistamines;

Skeletal Muscle Relaxant;

Generalized sedative action and altered pain perception;

Oral admin - drug levels ↑ with high fat meals*;

Tx: Muscle spasm;

SE: ↑ LFTs (monitor), N/V/GI upset, drowsiness, HA, irritability;

Interactions: Additive CNS depression;

Skeletal Muscle Relaxant;

No direct effects - generalized sedation and pain relief dt altered pain perception;

Oral, IV, or IM admin;

Tx: Muscle spasm, tetanus;

SE: Drowsiness, dizziness, bulrred vision, N/V, HA, irritability;

Interactions: additive CNS depression;

Skeletal Muscle Relaxant - related to diphenhydramine;

No direct effects, generalized sedative = analgeisic, mildly anticholinergic, antihistiminergic, local anesthetic actions all seen;

Oral, IV, or IM admin;

Tx: Muscle spasm and off-label use to tx Parkinson's;

SE: Xerostema, agitation, blurred vision, constipation, drowsiness, dizziness, N/V, HA, ↑ intraocular pressure*, mydriasis, urinary retention:

Interactions: Additive CNS depression, additive anticholinergic axns (esp on GI, bladder, eyes and temp and esp with TCAs, 1st gen antihistamines, and amoxapine);

Can also tx spasticity;

Presynaptic α2-agonist, ↓ sympathetic outflow from the CNS;

Tx: Hypertension and Spasticity;

Can also tx spasticity;

GABA analog, antiepileptic drug;

Can also tx spasticity off-label;

Prevents docking and release of neuronal vessicles containing Ach = interruption of nerve conduction and chemical denervation;

IM admin to tx spasticity;

Action may take weeks to set in but lasts for months;

SE: rash, puritis, allergic rxn, dystonia, dysphagia, URI, flu-like sx, rhinitis, muscle atrophy;

Ab formation at high doses (switch subtypes);

Interactions: Potentiation of axn when given with other drugs acting at the NMJ (AMG, chloroquine, NM blockers);

(Lyrica) - related to seizure med gabapentin;

Analog of GABA that binds to the alpha-2-delta subunits (covalently bound) of calcium channels where it ↓ neuronal calcium currents alleviating neuropathic pain, anxiety, and pain syndrome sx;

Oral admin;

Adjust dose with decreased renal fxn;

Only drug FDA approved to Tx Fibromyalgia;

SE: Sedation, dizziness, blurred vision, xerostomia, weight gain*, swelling of the hands and feet*;

Additive sedation with other CNS agents;

Ibuprofen,

Ephedrine,

Pseudoepehdrine

Epinephrine,

Phenylephrine,

Theophylline