Benzodiazepam

Benzodiazepam

Hypnotic

Flumazenil

GABAa receptor antagonist

Benzodiazepam OD antidote

Other CNS depressant

GABA receptor agonist

Hypnosis

No REM disturbance

CNS depressant

Anxiolytic

Acts on serotinin receptors

NO additive effects other CNS depressants

Barbiturate

ultrashort acting

Barbiturate

short acting 

Anxiolytic

Epileptic

Phenobarbital

Long acting barbiturate

tonic-clonic antiepileptic

Opioids

Narcotic Analgesics

CNS depressant + analgesic

Naloxone 

Blocks effects of narcotic analgesics

(opioids) use in case of OD

Like naloxone

Used to counter alcohol abuse

Narcotic Analgesic

CNS depressant

High dependence

Natural

Heroin

Semi-synthetic Narcotic analgesic

Highest dependence liability of opioids

More potent than morphine but not more efficacious

Mixed effect opioids

Without morphine: Get similar effect to other opioids

With morphine: Blocks the effects of morphine

Phenothiazine

(chlorpromazine)

Antipsychotic (high dopamine)

Blocks dopamine in limbic system (emotion)

Stops secondary messenger pathway for cAMP

reduces the available Nts 

Antipsychotic

Higher extrapyramidal effects 

Competitively blocks dopamine

Clozapine

Risperidone

Olanzapine

Atypical Antipsychosis

treats + and - symptoms schizophrenia

Lower extrapyramidal

blocks dopamine and serotinin

Mood Stabilizer

Blocks IP2--> IP and IP--> I

reducing PIP2, lowering IP3 + DAG so they can't have and effect (stimulate alpha adrenergic receptors)

Antidepressants 

Block serotinin + norepinephrine uptake

(depression = low serotonin + norep)

SSRI

Selective serotinin Reuptake Inhibitor

Stops the uptake of serotinin by inhibiting the serotinin transport proteins 

Fluoxetine (prozac)

SSRI

(prozac)

Inhibits serotinin transport +reuptake

Antidepressant

Inhibit degredation of:

MAO-A: serotinin, norepinphrine, tyramine

MAO-B: dopamine

Non-selective: Tranylcypromine + phenelzine

Selective MAO-A: Moclobemide

Methylphenidate

ALDH inhibitor in Alcohol biotransformation pathway

makes the person feel sick if they have alcohol because it isn't metabolized properly

ALDH inhibitor 

--> See disulfram 

CNS depressant

Low dose: increases GABA release 

High dose: Non selective inhibition excitable cells

Anandamide

THC endogenous ligand

involved in learning + memory

inhibits release Nts 

Nitroglycerine

Antianginal

Organic Nitrate - SHORT acting

Converted to NO in blood vessel

Causes vasodilations:

-veins: increase blood storing = decrease O2 req. 

-Coronary arteries = increase O2 supply

Long acting

Organic Nitrate

Antianginal

Vasodilation

Beta blocker

Antianginal

(beta adrenergic sympathetic)

Reduces heart contraction force = reduce O2 need

Calcium channel blocker

Inhibits the calcium-calmodulin complex from forming by reducing the amount of calcium in the cell

 The C-C complex would activate myosin kinase and this would bind myosin to actin causing a contraction but since no complex no contractions therefore less O2 req. 

Congestive Heart Failure Drug

cardiac glycoside

Digoxin = drug of choice

Binds to Na+/K+ ATPase to inhibit sodium's exit from the cell which makes calcium come into the cell

=Increased force heart contraction

Low safety margin

Can fix arrythmias

Type of digitalis

Congestive heart failure

cardiac glycoside

Increase force of heart contraction

from Digitalis lanatua plant

Largest lipoprotein

carries dietary triglycerides

Formed in intestine

Very low density lipoprotein

brings triglycerides from liver to body tissue

not good

LDL

BAD lipoprotein 

in blood

fatty deposits in arteries once taken up by macrophages

HDL

GOOD lipoprotein 

Carries triglycerides from arteries to the liver to be biotransformed + excreted 

Protect against heart disease

Use when high LDL

Insoluble (+) resin that binds (-) bile salts containing triglyerides

Stops their reabsorption - excreted

Increases secretion of bile salts so the liver has to take LDLs from the blood stream to make more

Gemfibrozil

Athlosclerosis (reduce cholesterol)

Use with high VLDL = high triglycerides 

Increases breakdown of triglycerides 

Inhibits VLDL release from liver

DO NOT use for combined hyperlipoproteinemia 

just if high VLDL

Niacin

Use with high VLDL 

Inhibits secretion of VLDLs from liver

This reduces LDLs as well 

MOST EFFECTIVE for INCREASING HDL

-Statins

(lovastatin)

Inhibits the enzyme (HMG CoA reductase) controlling the rate determining step in cholesterol biotransformation

basically cholesterol excreted faster

MOST EFFECTIVE at REDUCING LDLs and TOTAL CHOLESTEROL

alpha globulin ---renin---> angiotensin I ---ACE---> Angiotensin II ----> Vasoconstriction or Aldosterone release

Aldosterone secreted from adrenal cortex: causes increases salt and water reabsorption from the kidneys

INCREASE BLOOD PRESSURE

Hydrochlorothiazide

-thiazides 

Antihypertensives

Diuretics 

Increase salt + water excretion from kidney

Decreases resistance

Decreases BP

Effacacious alone or in combination 

Thiazides

Antihypertensives 

Reduce sympathetic NS Activity

antihypertensive

Beta blocker 

reduces heart contractions

BUT block beta receptors in bronchi causing spasms so can't use in asthamtics 

Also used as an antianginal

Reeduce sympathetic NS Activity

antihypertensives

vasodilation 

Reserpine

Reduce sympathetic NS Activity

antihypertensives

Destroys storage vessicles in adrenergic neurons (symp) (norepinephrine)

reduces signals = reduce BP

Reduce sympathetic NS Activity

antihypertensives

Centrally acting

Stimulates alpha adrenergic neurons in brain stem which decreases sympathetic stimulation of heart 

Vasodilator

Antihypertensive

Unknown mechanism

Vasodilation arterioles + coronary arteries

Antihypertensive 

ACE Inhibitor

Stops Angiotensin I --\\\\--> Angiotensin II 

Nifedipine

Calcium channel blocker

Antianginal + Antihypertensive

Stops calcium reaching smooth muscle so no vasodilation

Antibiotic

related to D-alanyl-D-alanine for building bacterial cells walls 

Protoplast = bacteria without cell wall, will burst

Combination antiobiotic

like penicillina

Amoxicillin + clavulinic acid

Resistance against penicillinase 

combination antibiotic

Sulfamethoxazole + Trimethoprim 

Anitfungal

Binds to ergosterol in fungus membrane

Creates pores - leaky

Need IV

Kidney toxicity