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All pharm 1
CNS and all others
149
Anatomy
Professional
09/17/2014

Additional Anatomy Flashcards

 


 

Cards

Term
Class IA
Definition

Fast fibers

Quinidine poster child

 Procainamide: slow acetylators are prone to lupus like

 Disopyramide: stronger anticholinergic


SVT( need digoxin)** , VT


Blocks Na--> long phase 0, ^APD, ^ ERP in fast fibers

Unlike other class I this one prolongs Action potential

Pro: M antagonist (speeds AV**, prolongs QRS, prolong QT which may cause torsades) a1 antagonism (reflex tachy)


Side effect: Cinchonism (due to M, a1 antagonism) : ocular disfunction w/ diplopia, GI distress, tinnitus, vertigo

Term

Class IB

 

 

least proarrythmic of all

Definition

Lidocaine IV

 Mexiletine oral

 

Hypoxia--> low ATP--> low Na/K ATPase activity--> ^ Na in cell--> ^ automaticity, long depolarization, low refractory, slow conduction

 

blocks Na inactivated channels: raised AP threshold

blocks late window Na channels: shortens APD, weak inhibitor of pahse 0

 

use: Post MI, digoxin toxicity, open heart surgery

Term
Class IC
Definition

Flecainide

Propafenone

 

life threatening VT, refractory SVT

 

Strongest inhibitor of phase 0, no change in length of action potential  

too good = sudden death

Term
Class II antiarrhythmic
Definition

Propranolol (b1,b2 others are just B1)

Esmolol-IV

Acebutolol

 

lowers phase 4: lowers SA firing and AV conduction

 

Pro: AV block

 

Caution: asthmatics, Peripheral vascular disease, DM

Term
Class III
Definition

Amiodarone

(does it all, long T1/2 due to iodione so shitty)

 

Sotalol

Dofetilide

Ibutillide

Dronedarone



Prolongs QT---> Torsade de pointe

Term
Class IV Antiarrhythmic
Definition

Verapamil

Diltiazem

 

 

Constipation

 

Term
Class V antiarrhythmics
Definition

Adenosine

DOC for paroxysmal supraventricular tachycardia

A1--> G1: lowers SA, A2a--> Gs vasodilate (even coronary), A2b--> Gq bronchoconstriction

 

Mg

polymorphic ventricular tachycardia (torsades)

Digoxin

Potassium Cl

digoxin toxicity (especially hypoK)

Term

Indications of Antiarrhythmic

 

SVT ( Sinus tachy, PSVT, atrial flutter)

 

AV block

 

Ventricular arrythmia ( tachy, torsades)

Definition

SVT ( II & IV, adenosine & all, all )

 

atropine

 

( all but IV, Mg & II IV)

Term
Testosterone vs DHT
Definition

LH --> leydig cell

 

FSH --> serotoli cell -_> estrogen

 

T: spermatogenesis (sertoli), muscle, ^ RBC, ^ bone

 

DHT: acne, bald, prostate, puberty changes

Term
Nadrolone
Definition

Anabolic steroid Testosterone derivative

 

 

Adverse: lower HDL, ^ LDL, ^ HR (- MAO), ^ RBC --> HTN, lower II,V,VII,X --> ^ PT, hepatic blood filled cysts, adenoma,  DM, gynecomastia, testicular atrophy, ^BPH, Teratogenic ( female fetus--- old people sex, female weight lifter)  

Term
Oxandrolone
(S)
Definition

Stanozolol

 

Anabolic steroid DHT derivative

Term
Finasteride
(D)
Definition

Dutasteride

 

5a reducatase inhibitor (no DHT)

 

BPH, hair growth

 

adverse antiadrogenic

Term
Ethinyl Estradiol
(M)
Definition

Mestranol

 

^ HDL, lowers LDL, blood clotting

 

Adverse: cigs + aging = clotting, cancers, gallstones

 

 

DES: In babies:  vaginal adenocarcinoma and in males hypospadia, cryptorchidism

Term
Raloxifene
Definition

SERM

 

partial agonist on bone

antagonist on breast,

agonist on endometrium

Term
Clomiphene
Definition

SERM

 

Blocks peripheral estrogen's negative feedback on GnRH, FS, LH

 

^ ovulation, multiple babies

Term
Norethindrone
(N,D)
Definition

Progestin

Norgestrel, Desogestrel

 

Precursor of androgen, estrogen, glucocorticoids

 

Adverse think PCOS: hair, acne, depress, DM like, ^LDL,lower HDL

Term
Hydrocortisone
Definition

cortisone ( 1:1)

short acting 1-12 hrs

 

 

Adverse of all glucocorticoids:

 

cushings ( ^ PEPCK* = gluconeogenesis oxaloacetate to phosphoenolpyruvate) , ACTH suppression --> adrenal cortical atrophy)

 

* glucagon, retinoic acid too

Term
Prednisone
Definition

Triamcinolone (4:1 salt)

inter 12-36

Term
Betamethasone
Definition

Dexamethasone

glucocorticoid

long 36-55 hrs

 

Term
Fludrocortisone
Definition

Mineralcorticoid

some glucocorticoid

Term

Dx of DM II

 

DM I trigger

 

MODY

 

control parameters

Definition

> 126 mg/dL on two separate occasion after overnight fast

 

> 200 mg/dL 2 hrs after 75 g oral glucose

 

DM 1: after coxsacie

 

MODY: mutations in glucokinase, insuline receptor, glucose transporter, nuclear transcription factors in beta cell gene expression

 

HB1c 7% or less, 150 mg/dl or less

Term
Canagliflozin
Definition

Sodium Glucose cotransporter 2 inhibitor in PCT

 

Adverse: ^ UTI

Term
Pramlintide
Definition

Amylin analog

 

delays gastric emptying--> lower appetite

Term
Miglitol
Definition

a-glucosidase inhibitor

Acarbose

Term
Sitagliptin
Definition

DPP-4 inhibitors (causing ^ GLP-1)

-gliptin

 

 

Adverse: Pancreatitis

Term
Exenatide
Definition

GLP-1 agonist

 SubQ

 

Liraglutide

 

^ I, lower Glucagon, delays gastric emptying

 

Adverse: Pancreatis*, ^ medullary carcinoman thyroid (MEN2, amyloid histo)

 

*Didanosine, stavudine, valproate, aspirginase

Term
Pioglitazone
(R)
Definition

Thiazolidinediones

Rosiglitazone

 

PPAR-y agonist

 

lowers liver gluconeogenesis, similar to metformin

 

Adverse: Edema+ weight gain --> ^^ CHF, bladder cancer (pio), angina & MI (rosi)

Term
Glipizide
(G,R)
Definition

Sulfonylureas 2nd gen

Glyburide,Repaglinide  Glimepiride, Glibenclamide


Glipizide: lower dose  in bad liver


Glyburide: lower in bad kidney


Repaglinide: no allergy

Term

Chlorpropamide

(A,T,T)

Definition

Sulfonylureas 1st gen

 

Acetohexamide, tolbutamide, tolazamide, SIADH** in chlorpromide

 

High plasma protein binding

blocks ATP-dependent K channels* in beta cells--> ^ insulin which lowers glucagon

 

Adverse: Hypersensitivity (rash, sulfa, hematological toxicity) , hypoglycemia, weight gain

 

* opens: thiazide, diazoxide, minoxidil

** also carbamezapine, inhibited by Li

Term
Metformin
Definition

oral

 

No hypoglycemia or weight gain

 

^ GLUT4, lowers PEPCK through AMP-Kinase

 

 

Adverse: lowers absorption of folate, B12, lactic acidosis

Term
Short acting Insulin
Definition

Glulisine (shortest), Lispro, Aspart

 

O: 15 min

 

D: 3-4 hrs

 

MOA: tyrosine kinase--> PI-3 kinase or MAPK

muslce, adipose: ^ GLUT 4

liver, muslce: ^ FA synthesis, ^VLDL,^ LPL, ^ glycogen, ^ glycolysis lowers FA & AA --> ketones, lowers gluconeogenesis

 

**  M, B2 = ^ insulin release

a2= lowers insulin

Term

Human insulin

 

(regular)

Definition

O: 30-60 mins

 

D: 6-8 hrs

Term
Intermediate Insulin
Definition

Human (no allergy potential) NPH

 

O: 2-4 hrs

 

D: 10-20 hrs

Term
Long acting
Definition

no peaks

 

Glargine, Detemir

 

O: 1.5 hr

 

D: detemir 17 hrs, Glargine 24 hrs

 

 

Term
Levothyroxine
Definition

T4

Permissive actions on B receptors (like cortisol)

Permissive action on ovarian cycle and spermatogensis

^ 02 consumption, ^ temp

^ gut motility and glucose absorption

Needed for carotene--> vit A

 

hypo:  hashimoto, amiodarone (hyper too), lithium)

Term
Methimazole (P)
Definition

Thyroid peroxidase inhibitors by inhibiting oxidation of Iodine to Iodide (1st step)

 

Propylthiouracil (prego): higher protein binding, also peripherally inhibits T4-->T3

 

Adverse: maculopapular rash, agranulocytosis

Term
Propranolol
Definition

Beta blocker and blocks deiodinase (t4-->T3)

 

inital drug for storm

Term
Alendronate
Definition

Bisphosphonates (dronates)

 

analog of pyrophosphate--> Stabilize hydroxyapatite--> inhibit osteoclast

 

AdverseL Osteoneocrosis of jaw, GERD--> esophageal adenocarcinoma

Term
Calcitonin
Definition

Inhibits osteoclastic bone resorption

 

Intranasal spray

 

Postmenu osteoporosis, HyperCa of malignancy

Term
Teriparatide
Definition

PTH analog

 

 ^ osteoblast vs continous administration --> ^ osteoclast

 

^ osteosarcoma

 

May cause ^ Ca avoid glucocorticoids, thiazides

Term
Denosumab
Definition

Against RANKL (osteoblast)  whch activates RANK on osteoclast

 

SubQ

 

mimicks osteoprotegerin ( ^ by estrogen)

Term
Cox 1 vs Cox 2 vs Lox
Definition

all act on g protein

LOX: leukocytes, mast cells, DO-- think asthman, anaphy

 

LTB4 - NO chemo, LTC-D4: ^ permeability, ^ mucus

 

cox1: continuous production in most cells,

cox2: induced in sites of inflammation, brain, kidney, PGI2 made by cox2

 

SS (vessel, airways, uterus):

^ conc PGD2, PGE2, PGI2 = relax

low conc: TXA2, PGF2A, PGE2 = constriction

 

Platelet:

high: PGI2,PGD2, PGE2 =stable

low: TXA2, PGE2* = Agg

 

* fever

Eye: PGE, PGF lower intraocular pressure, ^ outflow

 

Term

Aspirin

 

NSAIDs in general

Definition

Only NSAID that is irreversible of cox1,2 (acetylation of serine OH) & ETC uncoupler

 

300mg for pain, fever... grams for anti- inflamm

 

low: ^ uricemia

high: low urecemia bc damage to kidney

 

Toxicity:

uncouple--> ^ 02 consumption--> resp alkalosis--> ^ krebs--> ^ CO2--> >M acidosis

 

very low ATP--> NMJ depression--> low resp--> resp acidosis + M. acidosis --> Massive acidosis

 

Tx: drug is acid so alkalinize urine (acetazolamide)

 

Side effects:

       cox shutdown--> ^ LOX (avoid in asthmatics)

       Hypersensitivity

       Analgesic Nephropathy

       Salicylism ( tinnitus, vertigo, 1st sign)

       Reye: uncoupling--> multiple organ failure

 

Drug-drug:

    ^ bleeding with warfarin, ethanol

    sulfonylureas, warfarin --> ^ free conc

   Methotraxate not cleared by kidney

 

Ketorolac best analgesic

Indomethacin best anti-inflamm

Sulindac: easier on kidney, liver clearance

     

Term
Zileuton
Definition

inhibits 5-LOX

 

asthma prophylaxis

Term
Montelukast
Definition

Zafirlukast

 

 LTD4 receptor antagonist  ( mucus, permeability)

 

asthma prophylaxis

Term
Misoprostol
(A)
Definition

PGE1 analog

 

Alprostadil

 

NSAID ulcers, maintains PDA,

 

Abortion: mifepristone (anti-progestin)  + misoprostol

Term
Epoprostenol
(I,T)
Definition

PGI2

Illoprost, Treprostinil

 

Pul HTN

Term
Latanoprost
Definition

PGF2a analog

--prost

 

glaucoma, brown iris

 

 

Term
Dinoprostone
Definition

PGE2

 

Induce labor, abortion, hydatidiform mole,

Term
Celecoxib
Definition

COX-2 inhibitor

 

lowers PGI2 --> ^ MI, stroke

Term
Acetaminophen
Definition

central COX inhibitor (safe even in gout)

 

analgesic, antipyretic only

 

Hepatotoxicity: 10 g or P450 inducer (34A) makes N-acetyl-p-benzoquinone imine (NAPQI) damage to liver

 

Tx: N- acetylcysteine (mucus lytic, Tx: hemo cystitis cyclophosphamide)

 

 

 

 

Term

Histamine

 

H1 vs H2 vs H3 receptor

Definition

made from histidine, deactivated by MAOB

 

H1 (Gq) aka shock and anaphylaxis:

Broncho SS--> ^ Ca --> contract

P. nerves--> pain,  itch

AV node: lowers conduction

endo= ^ NO synthase, dilate, ^ Ca--> pericyte contraction, ^ permeability

CNS: wakefulness- pituitary, excites in cortex (reason for sedation and CNS depression with antihistamines)

 

H2: gastric parietal cells, cardiac, SS, mast cells

^ SA node firing, ^ contract of heart fast fibers

 

H3: presynaptic inhibition, lowers all neurotransmitters

Term
Diphenhydramine
(D,C)
(en/ine) or (en/ate)
Definition
dimenhydrinate, Chlorpheniramine

H1 blocker

 

Antimuscarinic action: motion sickness, parkinson, EPS from antipsychotics, cold meds dry secretions

 

H1 blocker: allergy, rhinitis, urticaria, sleep

Term
Cetirizine
(L,F)
Definition

Loratadine, fexofenodine

 

dont corss BBB so not sedative, no muscarinic

 

 

 

2nd gene H1 blockers

Term

Sucralfate

 

Stomach cytoprotectants ( 2more)

Definition

prodrug, needs acid to make bandaid

 

Bismuth Subsalicylate: same as above but not prodrug

 

Misoprostol: PGE1 (lowers acid, ^ HCO3, mucus)

Term
H. pylori Tx 2 combos
Definition

Omeprazole + clarithromycin ( Macrolide with less GI upset) + amoxiciilin

 

Bismuth + metronidazole (metallic taste, no alcohol) + tetracycline

Term

Antiacids

 

AlOH vs MgOH vs Ca-carbonate vs Na HCO3

Definition

chelates tetracyclines

 

Al: constipation

 

Mg: diarrhea

 

other too: may cause alkalosis

Term
Cimetidine
Definition

competitive H2 receptors antagonist

histamine is paracrine from enterochromaffine like cells

 

Nizatidine, Famotidine, Ranitidine

 

Cimetidine inhibites CYP450 and lowers androgen

 

 

Term
Omeprazole
Definition

PPI

 

irreversible H/K ATPase

 

DOC in severe GERD

 

Adverse:

 competes for CYP450 ( warfarine)

inhibits 2C19: ^ phenytoin

Induces 1A2: lowers imipramin, antipsychotics, theophylline

malabsorption of Fe, B12, ^ enteric, resp infections

Term
Serotonin
Definition

G.I cells, neurons, platelets

Tryptophan, MAOB--> 5-hydroxyindole acetic acid 5-HIAA

 

5HT1a (Gi) - run of the mill anxiety

5HT2a (Gq)-  action of atypical antipsychotics

5ht3(Na/K channel)-  antiemetics

4 (Gs)

Term
Cyproheptadine
Definition

5HT blocker in all suntypes

 

 

Carcinoid syndrome

 

also give Octreotide (somatosatin: halts serotonin secretion)

Term
Ondansetron
Definition

5H3

 

antiemetic

Term
Sumatriptan
Definition

5HT 1B/1D agonist (Gi)

 

vasocontriction

Presynaptic inhibitor of substance A, neurokinin A, CGRP

 

Tx: migraine

 

C/I: cardio or cerebrovascular disease

Term
Methysergide
Definition

5-HT2 blocker

 

 

Prophylaxis Migraine - 2nd line ( retroperitoneal fibrosis)

Term
Ergotamine
Definition

partial agonist at a1, 5HT2 receptor

 

vasoconstric

 

Migraine

 

 

Adverse: ischemia, abortion

Term

1st line prophylaxis of Migraine

 

BB, TCA, anti-seizures, Ca

Definition

Propanolol

Amitriptyline

Valproate, topiramate

Verapamil

Term

Omalizumab

 

 

 

Zileuton- good for asthma induced by aspirin

Zafirlukast treat asthma too but associated with Churg Strauss

Definition

humanized IgE ( precents mast cell activation)

 

 

unresponsive asthma

 

 

Term
Cromollyn Na
Definition

Nedocromil

 

 

Prevents degranulation of mast cells: lowers Histamine, leukotrienes

 

OTC seasonal allergies

Term
Theophylline
Definition

Phosphodiesterase ( ^ cAMP)

Any drug that targets bronchoconstriction = early response

 

antagonist of bronchonstrictive adenosine

 

Adverse: narrow therapeutic window, cardiac arrhythmias

 

2nd line asthma, apnea with prematurity

Term
-2Muscarinic antagonists for Asthma -2
Definition

Ipratropium- short

Tiotropium- long

 

DOC in beta blocker induced bronchospasm

Term

Betta 2 agonists for Asthma -2

 

short vs long acting

Definition

 

Acute Bronchoconstriction

Short:  Albuterol, Terbutaline

 

Prophylaxis of exercise induced asthma (must be in combo with steroid, solo can cause asthma attack)

Long: Salmeterol

Term

Asthma Corticosteroids

 

Inhaled (3) vs Systemic (2)

Definition

early and late response

 

Inflammation, prevents B2 from desensitization

 

Chronic treatment

Inhaled: Budesonide, Beclomethasone, Fluticasone

 

Only to bring asthma under control

Systemic: Prednisone (O), Prednisolone (IV)

 

 

 

Term
Acute Attack of Gout
Definition

NSAID: Indomethacin, Naproxen, Sulindac

 

Colchicine: tubulin, neutrophil mobility, activity

 

Steroids : if allergic to NSAIDs

Term
Prophylaxis of Gout
Definition

Xanthine oxidase inhibitors: Allopurinol*, febuxostat

* Steven-J, a prodrug .... Inhibits metabolism of 6-mercaptopurine (cancer)  and prodrug azathioprine (immunesupress)

 

Probenecid: inhibits reabsorption

 

Pegloticase: enzyme = uric acid--> allontoin , long term management of gout not responding to other therapiies

Term
Drugs associated with TNF- a
Definition

Infliximab: human  Ig-TNF-a

Adalimumab: human Ig-TNF-a

Etanercept: site for TNF receptor and has IgG Fc region

 

 

Reactivation fo HBV, TB

Term

DMARDs

 

MTX

Hydroxychloroquine

Sulfasalazine

Leflunomide

Rituximab

Penicillamine

Auranofin

Definition

- MTX:

DHF reductase inhibitor, lowers BM

 

- Hydroxychloroquine:

lowers RF, acute phase proteins,cinchonism, G6PD hemolysis. use in malaria, SLE,

 

- Sulfasalazine

 lowers b cell, inhibits COX, G6PD hemolysis

 

- Leflunomide


inhibits dihydroorotate dyhydrogenase in mito--> low UMP--> no ribonucleotide synthesis , arrests in G1, BM supression and liver toxicity can be fatal


- Rituximab

 CD20, used in B cell leukemias.. Can reactivate HBV, JC ( progressive multifocal leukoencephalopathy)

 

- Penicillamine

 Chelator of metals inhibits metalloproteases, supresses T lymphocytes, used in wilson


- Auranofin

lowers lysosomal and macro function, skin rash and mouth sores

Term

Immunosupression Drugs (anti-rejection drugs)

 

Cyclosporine

Tacrolimus

Sirolimus

Mycophenolate Motefil

Definition

Calcineurin cleaves P from NF-AT and frees it

 

- Cyclosporine:binds cyclophillin, inhibits de-P. no IL-2,y-IFN broken down by 3A4... nephro, neuro toxic, gingival hyperplasia ( Phenytoin, Ca channel dipines)

 

- Tacrolimus:  binds FK binding protein, inhibits de-P, used in Autoimmune

 

- Sirolimus/ rapamycin: Inhibits mTOR (in pathway involved in response to IL-2)   use in kidney transplant, coating cardiac stents, interstitial pneumonitis

 

- Mycophenolate Motefil: inhibits Inosine 5 monophosphate dehydrogenase --> no guanine, B,T cells cant use scavenger pathway, opp. infections

Term

GABA

 

&

 

Its Receptors

Definition

Makes: L-glutamic acid decarboxylase: glutamate + B6

Breaks: GABA transaminase: glutamate + succinic

 

Channel: 2 a, 2b, 1 y (2 gaba bind at a-b, BZ at a-y, Barbiturate at B)

 

GABA-A (GABA-C same): ligang gated, Cl in (BZ, barbs)

 

GABA-B: Gi (lowers cAMP), ^ K out, Ca in (baclofen)

Term

Benzodiazepine Profile

 

Antagonist?

Definition

allosteric at GABA-A, increases frequency (potentiation 0+1=2)

 

subunits:

a1,a5: sedation, ataxia, amnesia

a2,a3: anxiolysis, anti seizure

 

Acitve metabolites through 3A4, 2C19

 

Flumazenil antagonist: cant antagonize alcohol or barbiturates

 

 

Term

 

Short Acting

 

Anxiolytic 2

 

vs

 

Sedative

 

Benzo 1

 

TOM

Definition

Midazolam: anterograde amnesia, induce anesthesia

Oxazepam

 

vs

 

Triazolam

Term

Intermediate

 

Anxiolytic 3

 

vs

 

Sedative 2

 

Benzo

 

TALE

Definition

Alprazolam- Only one used in Anxiety associated with depression

Lorazepam- anterograde amnesia, status epilepticus

 

Chlordiazepoxide

 

vs

 

Temazepam

Estazolam

Term

Long acting

 

Anxiolytic 3

 

vs

 

Sedative 2

 

Benzo

 

DCC FQ

Definition

Diazepam- status epilepticus

Clonazepam

Clorazepate

 

vs

 

Flurazepam

Quazepam

Term
Zaleplon < Zolidem < Eszopiclone
Definition

not benzo but reverse by flumazenil

 

parasomnia

Term

Phenobarbital

(T, P

Definition

Primidone and phenobarbital: anticonvulsant

Thiopental : anesthetic

Pentobarbital: induce coma

 

Seizures

Increase DURATION of opening, block complex I of ETC

1st line neonates

cardioresp depression

 

 

Inducers of CYP450

Primidone is metabolized to phenobarbital and phenylethylmalonamide--all are anticonvulsants= severe sedation

Term
Buspirone
Definition

partial agonist 5HT1A

 

Anxiolytic

 

C/I: with MAO inhibitors

Term
Ramelteon
Definition

agonist melatoning receptor Gi

 

no dependence

 

sleep

Term

Tonic Clonic (grand mal)

 

DOC

Definition

Phenytoin*

Carbamazepine*

Valproic Acid*

 

Term
Absence (petit mal)
Definition

Ethosuximide*

 

 

Valproic acid

Lamtrigine

Term
Status Epilepticus
Definition

Lorazepam

Diazepam: acute

Phenytoin/fosphenytoin: prophylaxis

Term
Phenytoin
Definition

DOC for prophylacxis of status elipticus

DOC tonic clonic

 

blocks inactivated Na voltage channels (like 1b)

 

Zero order Kinetics at therapeutc range

 

inducer of CYP450

 

Gingival hyperplasia, Hirsutism, SLE-like, fetal hydantoin syndrome, pseuolymphoma (cleft lip/palate, heart, microcephaly, no nails)megaloblastic anemia,

 

Interfers with folate, VitD

Term
Carbamazepine
Definition

bipolar

DOC: trigeminal neuralgia, simple, complex, tonic clonic

 

blocks inactivated Na channels

 

 

Neural tube defects, SIADH, Steven-J, Aplastic anemia

Term
Valproic Acid
Definition

DOC tonic clonic

bipolar, prophylaxis of migraine, myoclonic

 

MOA: inhibits GABA transaminase (vigabatrin) , Inhibits inactivated voltage gated Na channels, inhibits histone deacetylase inhibits T type Ca channels,

 

Not inducer of P450, inhibits 2C9

 

Alopecia, pancreatitis, thrombocytopenia, ^ Bleed time, neural tube defects

Term
Ethosuximide
Definition

DOC Absence seizures only  (burst of thalamic activity, during seizure nothing can arouse them except smell)

 

T type Ca channel blocker

 

adverse EFGHIJ

 

 

Term
Lamotrigine
Definition

all and absences seizures

bipolar

 

Blocks voltage gated Na channels

 

 

Term
Topiramate
Definition

Anticonvulsant, prohylaxis of migraine

 

 

blocks Na channels, ^ GABA action

carbonix anhydrase inhibitor

 

Kidney Stones

 

Phentermine(amphetamine) /topiramate: 1st drug for Obesity

 

 

 

Term
Felbamate
Definition

antiepileptic

 

NMDA blocker

Term
Nitrous Oxide
Definition

Inhaled General Anesthetic

 

Very high MAC: weak

B/G: .45 small so fast onset/recovery

 

not metabolized (breath out)

 

displaces 02, diffusional hypoxia


gas trapped in cavity no malg hyperthermia

Term

Methoxyflurane vs vs halothane vs enflurane

 

 

sevoflurane

Definition

Inhaled general anesthetic

 

MAC is small

 

 All malignant hyoerthermia

 

Methoxyflurane: nephrotoxcity  

Halothane: Hepatotoxicity

enflurane: seizures

 

Term
Propofol
Definition

IV general Anesthetic

All IVpreps include:sedate= midazolam or Dexmedetomidine (a2 agonist, CNS depress), Dry secretion = atropine

 

"milk"

Potentiates GABA-a

 

Propofol infusion syndrome:

Rhabdomyolysis--> renal fail--> metabolic acidosis, hyperK--> cardio collapse

Term

Methohexital


THIOPENTAL

Definition

IV general Anesthetic

All IVpreps include:sedate= midazolam or Dexmedetomidine (a2 agonist, CNS depress), Dry secretion = atropine

 

Potent, ^ lipid, redistribution, rapid

 

lowers intracranial pressure, GABAa enhancer ( duration)

 

Term
Ketamine
Definition

Noncompetitive antagonist of NMDA glutamate receptor

Phencyclidine

 

Dissociative anesthetic

 

Adverse: vivid dreams and hallucination

 

^ intracranial pressure,

 ^ BP, HR

Term
Etomidate
Definition

IV general anesthetic ( Fentanyl also in this class, not below comments)

 

 

10% adrenal suppression ( cushing syndrome Tx)

Term

Local Anesthetics

 

PK?

 

PD?

 

adjuncts needed?

 

esters vs Amides

Definition

Weak bases need alkaline solution--> binds from within, as a cation on inactivated Na channels

 

From increasing size, myelination:

C fibers--> Ao--> Ay--> AB--> Aa

 Pain--> temp--> touch--> pressure--> motor

 

X-caine vs x-i-x-caine  ( amides, i before caine)

plasma esterases (genetic poly, looks like PABA so hypersensitivity) vs Liver P450

 

Add vasoconstriction ( epinephrine a1, high dose, a2: spinal anesthesia lowers substance P release)

a2: Dexmedetomidine, clonidine

Cocaine doesnt need it has NE reuptake blockade can causes ischemia, HTN

Term
Tetrodotoxin
Definition

saxitoxin (marine toxins)

 

block the activated Na channel ( 1A like)

Term
Batrachotoxin
Definition

ciguatoxin

 

binds w/in channel, prevents Na inactivation

 

hallucinations

Term

Mivacurium

 

vs

 

Atracurium

Definition

Non depolarizing neuromuscular blockers

Pancuronium( antimuscarinic),Vecuronium longer acting

 

competitive antagonists at muscle nicotinic ACh receptor

acts on skeletal muscles only (not cardiac)

 

reversed with neostigmine

 

Mivacurium: shortest, plasma esterases, can release histamine

 

Atracurium: intermediate, spontanous inactivation to laudanosine--> lowers threshhold for seizures

 

 

Term

Succinylcholine

 

Train of Four pattern?

Definition

Neuromuscular blockers (depolarizing)

 

agonist of nicotinic receptors also at ANS ganglia, muscarinic receptors (so aka ACh)

 

depolarized ( augmented by AChE inhibitor)--> Desensitization (antagonized by AChE inhibitor)

 

Avoid with peeps with poor cholinesterase metabolism

 

TOF ratio= 1 no drug or phase 1 of depolarized

TOF ratio: < 1= non depolarizing block or phase 2

Term

Baclofen

 

vs

 

Dantrolene

Definition

Spasmolytic drugs (depresses CNS)

 

GABAb agonist = K in

 

vs

 

Binds Ryanodine receptor channel (RyR1)  blocking Ca release from sER in muscle, no effect on heart or smooth muscle (RyR2) , used in Malignant hyperthermi*

 

 

* AD mutation of RyR1 or Ca cant get back in sER--> massive contraction, lactic acidosis

Term

Opiod Peptides, receptors

 

supraspinal vs spinal

 

tolerance exceptions?

 

W/D?

 

Acute vs long term W/D treatment

Definition

u (mu most numerous), k, o

all Gi

 

Receptor on neuro body ( K out) vs presynaptic (block ca released, no exocytosis, no NE, substance P)

 

Spinal:  inhibition of ascending pathways at dorsal horn

Supraspinal: Stimulation of modulatory descending pathway at Midbrain periaqueductal gray

 

No tolerance to miosis and constipation

negative reinforcement addiction (removal = hell)

W/D: due to ^ NE, substance P = agitation, pupil dilation, tachy, HTN, diarrhea, central originating pain

 

Acute: Methadone, Clonidine (lowers ANS)

Chronic: methadone, Buprenorphine w/ naloxone

Term

Morphine

(prototype since potency: 1)

Definition

Resp depression: knocks out pCO2 in CNS, PNS pO2 sense low oxygen and maintain breathing, giving 02 to some one opiods--> resp depression

 

Opiod OD triad: coma, resp down, pinpoint pupils

 

vessel: vasodilation& venodilation, in peripheral due to histamine(flushing, pruritus) , in CNS due to ^ CO2--> ^ ICP

Morphine uses: pulmonary Edema (low preload), MI, diarrhea,

 G.I : constipation, give methylnatrexone, less peristalsis but more spasms (biliary colic)

cough suppression (Dextromethorphan: opiod like OTC)

^ ADH, ^prolactin, ^ GH, lowers LH

 

Term

Merperidine

 

potency: .3

Definition

mu agonist

 

stong antimuscarinic: tachy, no GI,GU spasms, no miosis (addict in plain sight)

 

 

 

 

 

 

Term

Methadone

 

 

Definition

mu agonist (slow kinetics)

 

blocks NMDA

 

Additive resp depression w/ heroin

 

 

( just recognize all ---hydrocodones, oxymorphones as mu agonists and abused)

Term

Alfentanil

Fentanyl

Remifentanil

Sufentanil

 

Definition

mu agonist

 

anasthetics

 

Term

Codeine

 

 

 

Tramadol

Definition

agonist, considered partial bc its weak

 

analgesia w/ NSAIDs

 

antitussive

 

 

Tramadol: blocks reuptake of NE, 5HT ( seizures)used in neuropathic pain

Term

Loperamide

Dextromethorphan

Nalbuphine

Butorphanol

 

Definition

OTC opiods

 

Loperamide: diarrhea

Dextromethorphan: antitussive

 

Partial mu agonist and K receptor( dysphoria) antagonist  

Nalbuphine

Butorphanol

Pentazocine

 

Term

Naloxone

vs

Naltrexone

vs

Methylnaltrexone

Definition

IV

 

vs

 

oral, long acting in alcohol and opiate (lowers craving)

 

vs

 

cant cross to brain, SubQ for constipation due to opiod

Alvimopan (oral)

Term

Parkinsons

 

Levodopa/Carbidopa

Entacapone

Selegiline

Bromocritine

Benztropine

Amantadine

Definition

Levodopa/Carbidopa:

  precursore of dopamine/ peripheral carboxylase inhibitor

Entacapone:

  COMT inhibitor (catechol-methyltransferase)

Selegiline:

 MAOB inhibitor

Bromocritine:

 D2 agonist (hyperprolactemia,acromegaly)

Pramipexole, Ropinirole, Rotigotine 

 D3 agonist, antioxidant, antidepressant effects, also treats restless leg syndrome

Benztropine, Trihexyphenidyl

 muscarinic antagonists (lower tremor, rigidity)

Amantadine

 antiviral, ^ synthesis, release of DA, inhibits reuptake, inhibits muscarinic receptors

Term

Dopamine pathways in CNS

 

Nigrostriatal

Mesolimbic/cortical

Tuburoinfundibular

Definition

Nigrostriatal (pars compacta)

  - Output to striatum, D1 (gs) stimulates direct, D2(Gi) inhibits indirect , ACh (Gq) stimulates indirect..

 

Mesolimbic (reward, impusliveness) /Mesocortical (emotions, motivations)

 - same changes seen in addiction and schizophrenia

 - agonist: psychosis, euphoria   antagonist: opposite

 

Tuburoinfundibular

 - DA: lowers prolactin, GnRH, GH

 - antagonist: bitch tits with milk

Term

3 Theories on schizophrenia

 

Dopamine

Serotonin

Glutamate

Definition

Symptoms:

 (+) ^^DA in Mesolimbic : out to get me, hallucinations, (-) low DA in Mesocortex: fuck off, shitty speech, no emotion

 

Theories

Dopamine:

 less DA synthesis or release in limbic and cortex casues ^^ in DA receptors .. Typicals antagonis D2,D1 do nothing for (-) symptoms

 

 Serotonin:

  - 5HT inhibits DA release through 5HT2A receptors that are found in different densities.. Antagonism ^ DA and has the following effect:

   -  nigrostriatal: lowers extrapyramidal symptoms

   - Tuberoinfundibular: lowers hyperprolactemia

   - Mesocortical: improves (-) symptoms

   - Mesolimbic: D2 receptors >>> 5HT2A receptors so dont matter

   - Atypicals are weak D2 antagonist and strong 5HT2A blockers

 

Glutamate

 - NMDA receptors on GABA when stimulated suppress the brain.. Schizophrenia have shitty NMDA .. Future drugs

Term

Chlorpromazine

(prototype)

Definition

Blocks D2 receptors everywhere

 

Mesocortical: worse (-) symptoms

Mesolimbic: helps (+) symptoms

Tuberoinfundibular: ^ eating, bitch tits + milk

Nigrostriatal: ^ extrapyramidal symptoms (all give antimuscarinic w/ exceptions)

  -- early:

     - Acute dystonic: sustained contractions, twitching

     - parkinsons

     - akathisia: restlessness (crackhead, Tx: Benzo)

     - Neuroleptic malignant syndrome: catatonia, ^ fever, cardiodysfunction, myoglobinemia (Tx: halt medication, dantrolene, bromocriptine)

  --Late: (mo-> yrs):

     - Perioral tremors:

     - Tardive dyskynesia: irreversible, atypical dont cause this, due to ^ reg of D2 receptors

 

 

Adverse:

  Antimuscarinic: Coma,convulsion,cardiotoxicity(torsades)

  A1 antagonist: orthostatic hypotension, sexual dys

  H1 antagonist: sedation, weight gain

Term

Thioridazine

Fluphenazine

Haloperidol

Pimozide

Definition

Typical Antipsychotics

 

Thioridazine: strongest antimuscarinic (torsades)

Fluphenazine- depot form

Haloperidol- IV used in acute psychosis, mania

Pimozide- tourette syndrome, tic disorders  

Term

Clozapine

Olanzapine

Risperidone

Aripiprazole

Qutiapine

Ziprasidone

Definition

Atypical Antipsychotics

rule of thumb: Antagonist 5HT2A>> D2 (nigrastrital), antimuscarinic (seizures, dry mouth)

 

- Clozapine:  strong antagonists D4 (Mesolimbic). Agranulocytosis, hypersalivation, no EPS

- Olanzapine: only 5H2A, not as effective on (+),no D4

- Risperidone: a1 blocker

- Aripiprazole: D2 & 5HT1A (anxiety) partial agonist

     - also used for mania, autism

- Quetiapine: strong H1, a1 antagonism, no antimuscarinic

- Ziprasidone: blocks all DA, 5HT receptors and blocks 5HT, NE reuptake ---- powerful antidepressant

Term

Depression

role of neuroendocrine factors

&

Depression Hypothesis

 

Amine

Neurotrophic

 

Definition

Amine:

brain lacks amines: NE, 5HT, DA

Neurotrophic:

stress, pain--> lowers BDNF--> atrophy of cingulate (emotion, attention),  hippocampus, Meds ^ BDNF

 

Neuroendocrine factors:

Depression is seen in: ^cortisol, low estrogen, low testosterone, abnormal thyroid

Term

Tranylcypromine

Selegilline

Phenelzine

Isocarboxazid

Definition

 

irreversible MAOi

needs washout period if starting SSRI

 

Tranylcypromine: nonselective

Selegilline: MAOb, skin patch, ^ DA

Phenelzine: nonselective 

Isocarboxazid: nonselective

 

ATYPICAL ANTIDEPRESSION  

 

Term

MAOI

 

A vs B

 

diet drug restrictions

Definition

enzymes on outer mitochondrial membrane

A: neurons, liver, GI all neurotransmitters

 

B: neurons, platelets (DA, phenylethylamine = amphetamine actions)

 

Diet tyramine: soy sauce, sauerkraut, liver & meats, fava beans, alcohol, cheese

Tyramine displaces DA, NE, EP from vesicles

 

Drugs:

^ NE: TCA, a1 agonists (cold medications)

^5HT: St. johns wort, Dextromethorphan, meperidine, TCA

Term

Imipramine

Clomipramine

Amitriptyline

Amoxapine

Desipramine

Definition

TCA

block NE, 5HT reuptake

block a1, M, H1

metabolized by P450

Antagonism with a2 agonists (lowers NE lower Bp)

 

Imipramine: 5HT> NE, enuresis (lowers REM)

Clomipramine:  5HT>NE, OCD

Amitriptyline: 5HT=NE, neuropathic pain, migraine

Amoxapine: NE> 5HT, DA, psychotic depression

Desipramine: NE> 5HT, cocaine craving & W/D

Term

SSRI adverse

 

&

 

Serotonin syndrome, Tx?

Definition

 

GI: N/V, diarrhea

 

anorgasmia

 

CNS stimulate: insomnia, axiety ( intially give benzo)

 

platelets: ^ bleeds

 

Serotoning syndrom: rigidity, ^ temp, ANS dysfunction, myoclonus, coma Tx: Benzo, cyproheptadine (antagonist) or chlorpromazine

Term

Fluoxetine*

Paroxetine

Sertraline

Citalopram

Fluvoxamine*

Escitalopram

Definition

Powerful P450 inhibitors

Fluoxetine: 3A4 ( BZ/alprazolam, carbamazepine)

Sertraline: minimal inhibition

Citalopram: no inhibition

Fluvoxamine: 1A2 (TCA)

Paroxetine: 2D6 most potent, strong antimuscarinic, only one with no metabolite

Escitalopram

 

Term

Venlafaxine

Duloxetine

Milnacipran

Definition

SNRI

 

 

Duloxetone, milnacipran : fibromyalgia  (also pregabalin)

depression, neuropathic pain

Term

Nefazodone

Trazodone

Definition

Serotonin 2A antagonists* and reuptake inhibitors

SARIs

 

inhibits a1 (hypotension, arrhythmias, priapism

 

 

 

* (-) symptoms of mesocortex

 

 

Term
Mirtazapine
Definition

NaSSA

 

a2 antagonism: ^ NE synthesis, release

NE acitvate a1 in locus coeruleus --> ^ 5HT release

 

BLOCKS:

 - 5-HT2c, H1: weight gain (used in anorexia nervosa)

 - 5HT2A: no sex dysfunction

 - 5HT3: no N/V, GI

 - all available 5HT acts on 5HT1A ( anxiolytic like buspirone)

 

 

 

 

Term
Bupropion
Definition

atypical antidepressant

 

^DA, NE (blocks reuptake and enhance release)

 

 

smoking cessation too

Term

Bipolar I vs II vs III

 

Hospital acute Tx?

 

Definition

I: depressive, manic

 

II: depressive + hypomanic (cyclothymic)

 

III: Mania when treated with antidepressant for a depressive episode

 

Tx: Clonazepam

Term

Lithium

 

(behaves like Na)

 

alternative in Prego?

Definition

blocks inosine 5'- monophosphatase--> lowers inositol --> lowers Gq

stabilizes inactive trimeric G protein of Gs, Gi

inhibits PKC (synaptic plasticity)

 

Vd: 60% of weight

 

Competes with Na for reabsorption in PCT, small amount in DCT ( triamterene, amiloride* ^ clearance)

Diuretics decrease clearance

NSAIDs, ACE ^ reabsorption

 

Side effects due to depolarization: tremors (propranolol)

Side effects due to G protein:

  - ADH binds V2 receptors (Gs): polyuria, polydipsia* dont give thiazide ( Tx: Diabetes insipidus, would lower clearance)  

  - TSH binds (Gs): hypothyroid

  - glucose intolerance, leukocytosis

 

Teratogenic: Ebstein anomaly ( tricuspid leaflet points towards apex), large atrium, small ventricle, WPW

 

Lamotrigine

antipanic: Gabapentin, clonazepam

Term
Mood stabilizers
Definition

Valproate

Carbamazepine

Lamotrigine

 

Quetiapine, Olanzapine, Risperidone, Aripiprazole

Term

Amphetamine

MethylPhenidate

Atomoxetine

Cocaine

Bath Salts

Definition

Stimulants

Nacolepsy, Obesity, obstructive sleep apnea, ADHD

Amphetamine, Methylhenidate:

^ release of DA,NE, 5HT, block reuptake

Anxiety, HR,HTN, Mydriasis

Atomoxtine:

 - NE reuptake inhibitor

 -  Suicidal ideation, no abuse no W/D

 

Cocaine:

 - Blocks DA, NE, 5HT reuptake no effect on mobile pool

 - also blocks vol Na channel

 

Bath salts:

 - act like cocaine, amphetamine

 - violent, HTN,HR, hallucinations, seizures, rhabdomyolysis--> ARF... supportive

 

Term

CB1 vs CB2

 

Definition

Receptors both Gi

THC: CB1>CB2 agonist

endogenous from membrane phospholipids

 

Term

Methotrexate

5-flurouracil

Cytarabine

Mercaptopurine

Definition

Antimetabolites, S phase

 

Methotrexate

  - inhibits DHF redutase ( T,A,G), leucovorin

  - NSAIDS, penicillin ^ toxicity

5-flurouracil (IV) capecitabine (oral)

  - - thymidylate synthase after activation to FdUMP

   - hand foot syndrome, neurotox

Cytarabine

   - (-) DNA polymerase after its -P- and incorporated lookes like cytosine

Gemcitabine:

  - (-) DNA pol, (-) ribonucleotide reductase

Mercaptopurine

  - Activated by HGPRTase to monoP

  - (-) PRPP amidotransferase (Rate lining in de novo purine)

   - immunesuppression (azathioprine is prodrug)

 

Term

Cyclophosphamide

Cisplatin

Carmustine

Lomustine

 

Definition

Alkylating Agents (N7 guanine is most common site), ^ risk of leukemia, lymphoma

Not cell cycle specific

 

Cyclophosphamide

  - hemorrhagic cystitis due to acrolein, MESNA

  - If cystitis already give N- acetylcysteine

Cisplatin

  - Nephrotoxocity ( give amifostine), Severe N/V ( ondansetron), ototoxicity, P. neuropathy

Carmustine

  - Interstitial pneumonitits

 

Term

Vinblastine

Vincristine

Paclitaxel

Irinotecan

Topotecan

Etoposide

Definition

Vinblastine, Vincristine

  - M phase, inhibts microtubule polymerization, arrest in metaphase, P. neuropathies, no BMS with vincristine

Paclitaxel

  - Mphase, stabalizes microtubules, arrest in prophase, P. neuropathies,

Irinotecan

  - Sphase, inhibits topoisomerase I

Etoposide

   - sphase, inibits topoisomerase II

Term

Actinomycin D

Bleomycin

Daunorubicin

Doxorubicin

Definition

Antitumor antibiotics

 

Actinomycin D, a-manitin

  - (-) RNA polymerases, blocks transcription

Bleomycin

  - G2 specific, binds iron--> ^ ROS, pulmonary fibrosis

Daunorubicin, Doxorubicin

  - intercalates DNA, ^ ROS, blocks topoisomerase II

  - Red-orange urine, Cardio: acute= arrhythmia, chronic: dilated

  - Dexrazoxane chelates iron

 

 

Term

Tamoxifen

Fulvestrant

Anostrozole

 

Definition

Hormonal therapy cancer

 

Tamoxifen, Toremifene

   - SERM, (-) at ER in breast, (+) everywhere else

   - ^^ endometrial carcinoma, osteoporosis, lowers Cholesterol, LDL

Fulvestrant

  - pure ER antagonist and ^ degration of receptor

Anostrozole


   - competative inhibitor of aromatase

Exemestane

  - irreversible aromatase

 

Term

Rituximab

Trastuzumab

Cetuximab

Imatinib

Gefitinib

Eriotinib

 

 

Kill by ADCC, complement, induce apoptosis

 

Definition

Cancer antibodies

Rituximab

  - CD20, NHL, CLL (wegener, mico polyangiitis, ITP, R.A)

Trastuzumab

  - ErbB2 of EGF receptor, (+ metastatic breast, gastic, gastroesophageal adenocarcinoma)

Cetuximab

  - ErbB1 of EGF receptor in meatastatic colorectal cancer)

Imatinib

  - TK, bcr-abl (CML: 9,22), c-kit (G.I stromal), PDGFR (^ EO syndrome)

Gefitinib: ErbB1  non small cell lung cancer  

Eriotinib: same as above

Sorafenib, Sunitinib: many TK

Alemtuzumab

 - CD52(lymphocytes, PMN) , CLL,

Bevacivumab

 - VEGF, toxicity: HTN, CHF, proteinuria, G.I hemmorrhage

 - metastatic colorectal, non-small cell lung cancer, erbB2 (-) breast cancer

Term
L- Asparaginase
Definition

anticancer

 

Need asparagine--> aspartate + Ammonia

 

Toxicity due to lower protein synthesis: low insulin, less clotting factors, pancreatitis ( valproate, didanosine, stavudine)

Term
All trans retinoic acid
Definition

AML-M3 expresses vit-A receptor

 

forces differentiation of promyelocytes--> myelocytes--> metamyelocytes--> Bands--> PMN

 

Retinoic Acid syndrome: fever, dyspnea, effusions (lung, pleural, pericardial), mental confusion

Term
Hydroxyurea
Definition

Anticancer

 

S-phase

 

Inhibits Ribonucleotide Reductase (no ribnucleotide--> deoxyribonucleotide)

Term
Bortezomib
Definition

Binds 20S core of 26S proteasome

 

 

^ I-kB (inhibitor of NF-kB--> ^ cyclins, bcl-2,VEGF etc)

Term

Temsirolimus

Everolimus

Definition

mTOR inhibitors

 

inhibits PI3 kinase which activates mTOR

 

 

 

Term

Leuprolide

Degarelix

Flutamide

 

Definition

Leuprolide, Goserelin, Triptorelin

  - GnRH analog, block surge

Degarelix

  - GnRH antagonist

 Flutamide

   - Competitive antagonist

 

 

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