Cholinomimetrics

(Direct Muscarinic Agonist)

-M3 agonist (empty bladder+GI motile)

-Mild M2 agonist

(Slight decrease HR; Heart safe)

-Decreased CAMP

Cholinomimetrics

(Direct Muscarinic Agonist)

-M3 agonist (opto drops-constrict pupil

-decrease intraocular pressure; treat xerostomia

-Increase IP3/Ca2+

Cholinomimetrics

(Direct Muscarinic Agonist)

-NMJ and Autonomic ganglia

-Opens Na+/K+ channels

Cholinomimetrics

(Direct Muscarinic Agonist)

- ophthalmic purposes, such as for treatingglaucoma, or for use during ophthalmic surgery. It is generally administered as an ophthalmic solution (i.e. eyedrops).

- 

Cholinesterase inhibitors (Indirect Muscarinic Agonists)

 -so-called Tensilon test is used to differentiate myasthenia gravis from cholinergic crisis

Cholinesterase inhibitors (Indirect Muscarinic Agonists)

Parathion is a cholinesterase inhibitor. It generally disrupts the nervous system by inhibiting the acetylcholinesterase

Cholinesterase inhibitors

(Indirect Muscarinic Agonists)

-organophosphate parasympathomimetic which binds irreversibly to cholinesterase

Malathion in low doses (0.5% reparations) is used as a treatment for: head lice and body lice

Cholinesterase inhibitors

(Indirect Muscarinic Agonists)

-centrally acting reversible acetylcholinesterase inhibitor. Its main therapeutic use is in the palliative treatment of mild to moderate Alzheimer's disease.

Cholinesterase inhibitors

(Indirect Muscarinic Agonists)

-centrally acting anticholinesterase and indirect cholinergic agonist (parasympathomimetic). It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex.

Anti-muscarinic drugs (Muscarinic Antagonist)

-used to treat intestinal hypermotility, the symptoms of Irritable Bowel Syndrome (IBS) 

-Blocks M3?? Thus decreasing IP3/Ca2+

Anti-muscarinic drugs

(Muscarinic Antagonist)

long-acting, 24 hour, anticholinergic bronchodilator used in the management of (COPD)

-Blocks M3; thus decreasing IP3/Ca2+==>Brochodilating

Anti-muscarinic drugs (Muscarinic Antagonist)

-M3>M2>minimal M1

In anesthesia, glycopyrrolate injection can be used as a preoperative medication in order to reduce salivary, tracheobronchial, and pharyngealsecretions, as well as decreasing the acidity of gastric secretion. It is also used in conjunction with neostigmine, a neuromuscular blocking reversal agent, to prevent neostigmine's muscarinic effects such as bradycardia.

Anti-muscarinic drugs (Muscarinic Antagonist)

 -antimuscarinic agent used for the treatment of excessive sweating (hyperhidrosis), cramps or spasms of the stomach, intestines (gut) or bladder, and involuntary urination (enuresis)

-M3??

Anti-muscarinic drugs (Muscarinic Antagonist)

anticholinergic drug used for the treatment of chronic obstructive pulmonary disease and acute asthma. It blocks the muscarinic acetylcholine receptors in the smooth muscles of the bronchi in the lungs, opening the bronchi. ^[1]

Anti-muscarinic drugs (Muscarinic Antagonist)

-M₁,M₂,M₃

Anti-muscarinic drugs (Muscarinic Antagonist)

Scopolamine exerts its effects by acting as a competitive antagonist atmuscarinic acetylcholine receptors, specifically M1 receptors; it is thus classified as an anticholinergic, anti-muscarinic drug.

-Increase IP3/Ca2+

Anti-muscarinic drugs

(Muscarinic Antagonist)

used in eye drops as a cycloplegic, to temporarily paralyze accommodation, and as a mydriatic, to dilate the pupil.

Anti-muscarinic drugs (Muscarinic Antagonist)

Darifenacin works by blocking the M₃ muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions

-Increases IP3/Ca2+

Anti-muscarinic drugs (Muscarinic Antagonist)

used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination (urge incontinence), by decreasing muscle spasms of the bladder.^[ It competitively antagonizesthe M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor. 

Anti-muscarinic drugs (Muscarinic Antagonist)

The binding of acetylcholine to these receptors, particularly the M₃receptor subtype, plays a critical role in the contraction of smooth muscle. By preventing the binding of acetylcholine to these receptors, solifenacin reduces smooth muscle tone in the bladder, allowing the bladder to retain larger volumes of urine and reducing the number of micturition, urgency and incontinence episodes. Because of a long elimination half life, a once-a-day dose can offer 24 hour control of theurinary bladder smooth muscle tone.

Anti-muscarinic drugs

(Muscarinic Antagonist)

Anti-muscarinic drugs (Muscarinic Antagonist)

Pralidoxime attaches to the site where a cholinesterase inhibitor has attached, then attaches to the inhibitor, removing the organophosphate from cholinesterase, allowing it to work normally again. This is known as "regenerating" or "reactivating" acetylcholinesterase. After some time, though, some inhibitors can develop a permanent bond with cholinesterase, known as aging, where oximes such as pralidoxime can not reverse the bond

Adrenoreceptor Agonists

-alpha1>2-->Vasoconstriction=increased BP; Negative feedback on Vagus 

-Use: Tx paroxysmal a-tach, pressor agent; nasal congestion

Adrenoreceptor Agonists

-a sympatholytic medication used to treat medical conditions, such as high blood pressure, ADHD and anxiety/panic disorder. It is a direct-acting α₂ adrenergic agonist and a guanidine receptor agonist

-decrease CAMP

Adrenoreceptor Agonists

primary mechanism is direct stimulation of β₁ receptors

-Increases CAMP

Adrenoreceptor Agonists

use is for bradycardia or heart block. By activating β₁-receptors on the heart, it induces positive chronotropic, dromotropic, andinotropic effects.^[1]

It can be used as an inhaled aerosol to treat asthma, although this is currently a rare treatment.^[1] Although it activates all beta adrenergic receptors, it works in a similar fashion to the more selective β₂-adrenergic agonists

Adrenoreceptor Agonists

-Terbutaline is used as a fast-acting bronchodilator (often used as a short-term asthma treatment) and as a tocolytic to delay premature labor. The inhaled form of terbutaline starts working within 15 minutes and can last up to 6 hours.

-Beta-2; increases CAMP

Adrenoreceptor Agonists

bronchodilator used in the treatment of asthma. Orciprenaline is a moderately selective beta₂-adrenergic receptor agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle, with minimal or no effect on alpha-adrenergic receptors

Adrenoreceptor Agonists

• Dopamine induces  (sodium loss) in the , and has a diuretic effect, potentially increasing urine output from 5 ml/kg/hr to 10 ml/kg/hr. Dosages from 2 to 5 μg/kg/min are considered the "renal dose". At this low dosage, dopamine binds  receptors, dilating blood vessels, increasing blood flow to , , and arteries, thus increasing overall renal perfusion.natriuresiskidneys^[61][62][63]D₁renalmesentericcoronary^[64]

• Intermediate dosages from 5 to 10 μg/kg/min, known as the "cardiac dose", additionally have a positive  and  effect through increased  activation. Dopamine is used in patients with  or  to increase  and . Dopamine begins to affect the heart at lower doses, from about 3 μg/kg/min IV.inotropicchronotropicβ₁ receptorshockheart failurecardiac outputblood pressure^[64][65]

• High doses from 10 to 20 μg/kg/min are the "pressor dose".^[66] This dose causes vasoconstriction, increases systemic vascular resistance, and increases blood pressure through α₁receptor activation,^[64] but can cause the vessels in the kidneys to constrict to the point that urine output is reduced.^[66]

Adrenoreceptor Agonists

activating peripheral D_{1 (selective)} receptors, fenoldopam causes arterial/arteriolar vasodilation leading to a decrease in blood pressure. It is particularly effective in dilating the renal, mesenteric, and coronary arteries, where D₁.receptors are found

Adrenoreceptor Agonists

alpha-adrenergic agonist(selective for α₂-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive

-Preelcampsia; sever HTN

Adrenoreceptor Agonists

is an agonist of the α_2A subtype ofnorepinephrine receptors. These receptors are concentrated heavily in the prefrontal cortex and the locus coeruleus, with the potential to improve attention abilities via modulating post-synaptic α_2A receptors in the prefrontal cortex

Adrenoreceptor Agonists

nonselectively agonizes α1 and α2 adrenergic receptors.^[5] Since vascular beds widely express α1 receptors, the action of oxymetazoline results in vasoconstriction

Adrenoreceptor Agonists

increasing the activity of noradrenaline at the post-synaptic α- and β-receptors

Adrenoreceptor Agonists                                      

therapeutic effects via blocking the reuptake of dopamine into nerve terminals (as well as stimulating the release of dopamine from dopamine nerve terminals) resulting in increased dopamine levels in the synapse.^[102][108] The onset of central nervous system effects occurs rapidly after intake of methylphenidate 

Adrenoreceptor Agonists

Tyramine acts as a catecholamine (dopamine, norepinephrine (noradrenaline), epinephrine(adrenaline)) releasing agent. Notably, however, it is unable to cross the blood-brain-barrier (BBB), resulting in only nonpsychoactiveperipheral sympathomimetic effects.

Adrenoreceptor Agonists

muscle relaxant. It is a centrally acting α₂ adrenergic agonist

Adrenoreceptor antagonists

class of alpha-adrenergic blockers. Specifically, prazosin is selective for the alpha-1 receptors on vascular smooth muscle. These receptors are responsible for the vasoconstrictive action ofnorepinephrine, which would normally raise blood pressure and cause increase in anxiety and panic. By blocking these receptors, prazosin reduces blood pressure and reduces anxiety and panic.

Adrenoreceptor antagonists

selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It also acts to lower the blood pressure, and is therefore a drug of choice for men with hypertension and prostate enlargement.

Adrenoreceptor antagonists

α1a-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).

Adrenoreceptor antagonists

causes vasodilatation in blood vessels, due to its antagonistic effect at the alpha-1 adrenoceptor found in the walls of blood vessels, resulting in a drop in blood pressure. -Tx- Pheochomocytoma

Adrenoreceptor antagonists

reversible^[1] nonselective alpha-adrenergic antagonist

-Tx pheochromocytoma

Adrenoreceptor antagonists

It behaves as an antagonist at α₁-adrenergic, α₂-adrenergic, 5-HT_1B, 5-HT_1D, 5-HT_2A, 5-HT_2B, and D₂, and as a partial agonist at 5-HT_1A

Adrenoreceptor antagonists

a selective β₁ receptor blocker 

Adrenoreceptor antagonists

a sympatholytic non-selective beta blocke

Adrenoreceptor antagonists

an α_1a-selective alpha blocker used in the symptomatic treatment of benign prostatic hyperplasia (BPH).- (FLOMAX)

Adrenoreceptor antagonists

a selective β₁ receptor antagonist

Adrenoreceptor antagonists

 non-selective beta blocker/alpha-1 blocker indicated in the treatment of mild to moderate congestive heart failure (CHF)

Serotonin drugs

Sumatriptan is structurally similar to serotonin (5HT), and is a 5-HT (types 5-HT_1D and 5-HT_1B^[7]) agonist

Serotonin drugs

selective serotonin receptor agonist of the 1B and 1D subtypes

SSRI (prozac)

SSRI although it may produce some of its effects through 5-HT_2C antagonism 

SSRI (zoloft)

also a dopamine reuptake inhibitor, with a K_i=315 nM,^[152] a σ₁ receptor agonist with 5% of its SRI potency,^[153] and an α₁-adrenoreceptor antagonis

Dual Mechanism, "clean" drugs

 one of the few noradrenergic and specific serotonergic antidepressants (NaSSAs)

TCA

Amitriptyline acts primarily as a serotonin-norepinephrine reuptake inhibitor, with strong actions on the serotonin transporter, and moderate effects on the norepinephrine transporter.^[12][13] It has negligible influence on the dopamine transporter 

TCA

inhibits the reuptake of norepinephrine (noradrenaline) and, to a lesser extent, serotonin with negligible effects on dopamine reuptake

TCA

inhibits the reuptake of norepinephrine and to a lesser extentserotonin

Irreversible MAOI's

non-selective and irreversible monoamine oxidase inhibitor (MAOI)

Reversible MAOI's

is a selective irreversible MAO-B inhibitor, however in larger doses it loses its specificity and also inhibits MAO-A

Benzodiazepines

therapeutic and adverse effects by binding to the benzodiazepine receptor site on the GABA_A receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain

Benzodiazepines

its therapeutic as well as adverse effects via its interaction at benzodiazepine binding sites, which are located on GABA_A receptors in the central nervous system

Benzodiazepines

its therapeutic as well as adverse effects via its interaction at benzodiazepine binding sites, which are located on GABA_A receptors in the central nervous system

Benzodiazepines

action of diazepam enhances the effect of the neurotransmitter GABA by binding to the benzodiazepine site on the GABA_Areceptor leading to central nervous system depression.^[4]

Non-benzodiazepine anxiolytics or hypnotics

short-acting nonbenzodiazepine hypnotic of the imidazopyridine class ^[2] that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to GABA_A receptors at the same location as benzodiazepines

Non-benzodiazepine anxiolytics or hypnotics

Buspirone functions as a serotonin 5-HT_1A receptor partial agonist.^[9] It is this action that is thought to mediate its anxiolytic and antidepressant effects. Additionally, it functions as a dopamine D₂, as well as α₁, and α₂-adrenergic receptor antagonist to a lesser degree,

First generation Antipsychotics

works on a variety of receptors in the central nervous system, producing anticholinergic, antidopaminergic, antihistaminic, and weak antiadrenergic effect

First generation Antipsychotics

used primarily in the treatment of schizophrenia

First generation Antipsychotics

strong central antidopaminergic action, it is classified as a highly potent neuroleptic

Neuromuscular blocking agents

depolarizing neuromuscular blocker. It inhibits the action of acetylcholine at the neuromuscular junction

Neuromuscular blocking agents

 non-depolarizing curare-mimetic muscle relaxant. It acts as a competitive acetylcholine antagonist onneuromuscular junctions

Neuromuscular blocking agents

 neuromuscular-blocking drug or skeletal muscle relaxantin the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to provide skeletal muscle relaxation during surgery or mechanical ventilation.

Heart failure drugs

Digoxin binds to a site on the extracellular aspect of the α-subunit of the Na⁺/K⁺ ATPase pump in the membranes of heart cells (myocytes) and decreases its function. This causes an increase in the level of sodium ions in the myocytes, which leads to a rise in the level of intracellular calcium ions

Heart failure drugs

 is a phosphodiesterase 3 inhibitor. It potentiates the effect of cyclic adenosine monophosphate (cAMP).

Milrinone also enhances relaxation of the left ventricle by increasing Ca²⁺-ATPase activity on the cardiac sarcoplasmic reticulum

Heart failure drugs

Amrinone has been shown to increase the contractions initiated in the heart by high gain calcium induced calcium release (CICR)(9). The positive inotropic effect of amrinone is mediated by the selective enhancement of high gain CICR which contributes to the contraction of myocytes by phosphorylation through cAMP dependent protein kinase A (PKA) and Ca²⁺calmodulin kinase pathways(9).

Heart failure drugs

works to facilitate cardiovascular fluid homeostasis through counterregulation of the renin-angiotensin-aldoesterone system, stimulating cyclic guanosine monophosphate, leading to smooth muscle cell relaxation. (BNP analog)

Heart failure drugs

Spironolactone inhibits the effect of aldosterone by competing for intracellular aldosterone receptors in the cortical collecting duct. This decreases the reabsorption of sodium and water, while decreasing the secretion of potassium.

is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics  

Heart failure drugs

an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to the diuretic spironolactone, though it may be more specific for the mineralocorticoid receptor 

Heart failure drugs

 non-selective beta blocker/alpha-1 blocker indicated in the treatment of mild to moderate congestive heart failure (CHF)

Heart failure drugs

Pure artery dilator; ONLY VASODIALATES arteries; Pure afterload reducer.

Decreased mortality in African Amer. when used inconjunction with Beta blockers/ACE inhibt

Heart failure drugs

primary mechanism is direct stimulation of β₁ receptors

-Increases CAMP

Heart failure drugs

Losartan is a selective, competitive angiotensin II receptor type 1 (AT₁) receptor antagonist, reducing the end organ responses to angiotensin II.

Heart failure drugs

Olmesartan is a prodrug that works by blocking the binding of angiotensin II to the AT₁ receptors in vascular muscle; it is therefore independent of angiotensin II synthesis pathways, unlike ACE inhibitors. By blocking the binding rather than the synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion

Heart failure drugs

a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type β1 adrenergic receptor blocker.

Heart failure drugs

Furosemide, like other loop diuretics, acts by inhibiting NKCC2, the luminal Na-K-2Cl symporter in the thick ascending limb of the loop of Henle. The action on the distal tubules is independent of any inhibitory effect on carbonic anhydrase or aldosterone; it also abolishes the corticomedullary osmotic gradient and blocks negative as well as positive free water clearanc

Heart failure drugs

Conivaptan inhibits two of the three subtypes of the vasopressin receptor (V1a and V2). Effectively, it causes iatrogenic nephrogenic diabetes insipidus.

Heart failure drugs

is a selective, competitive arginine vasopressin receptor 2 antagonist used to treathyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH)

Heart failure drugs

L-type calcium channel blocker of thephenylalkylamine class. It has been used in the treatment of hypertension, angina pectoris, cardiac arrhythmia, and most recently, cluster headaches.

Heart failure drugs

a long-acting calcium channel blocker (dihydropyridine (DHP) class) used as an anti-hypertensive and in the treatment of angina. Like other calcium channel blockers, amlodipine acts by relaxing the smooth muscle in thearterial wall, decreasing total peripheral resistance and hence reducing blood pressure; in angina it increases blood flow to the heart muscle (although DHP-class calcium channel blockers are more selective for arteries than myocardium, as the cardiac calcium channels are not of the dihydropyridine-type).

Heart failure drugs

 is a dihydropyridine calcium channel blocker. Its main uses are as an antianginal (especially in Prinzmetal's angina) and antihypertensive

5HT1 Agonist(Imitrex)

Sumatriptan is structurally similar to serotonin (5HT), and is a 5-HT (types 5-HT_1D and 5-HT_1B^[7]) agonist

5HT1 receptor AGONIST (Zomig)

Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes

5HT4 receptor AGONIST (GI and esophygeal motility; dangerous for cardiac K+ channel)

Cisapride is a gastroprokinetic agent, a drug which increases motility in the upper gastrointestinal tract. It acts as a serotonin 5-HT₄receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases acetylcholine release in theenteric nervous system

5HT4 receptor AGONIST. (GI and esophageal motility;safer; bound to plasma proteins)

The drug functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT₄ receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain.^[3] Additionally, tegaserod is a 5-HT_2B receptor antagonist