An agent that stimulates the postganglionic parasympathetic receptor. Pure muscarine compared to pure acetylcholine is stated in most cases to be more potent, its action is always slower but longer lasting than acetylcholine. J Toxicol Clin Toxicol 1992; 30: 347-349. The symptoms of intoxication with mushrooms rich in muscarine, especially Inocybe, are very typical: Bronchoconstriction leads to asthmatic attacks and severe dyspnea, and bradycardia combined with marked hypotension and vasodilation results in circulatory shock. Pralidoxime – Nucleophilic agent that reactivates the phosphorylated AChE by binding to the OP molecule. A mixture of signs and symptoms can occur with muscarinic poisoning from medications or mushrooms. bronchorrhea). Stephen Haydock. 2004 May;26(4):429-32. doi: 10.1016/j.jemermed.2003.09.013. Tweet. Mushrooms in the genera Entoloma and Mycena have also been found to contain levels of muscarine which can be dangerous if ingested. Organophosphate poisoning can be short- or long-term. Figure 1. It can be caused by large or small doses. α-blocker physostigmine, a cholinesterase inhibitor. Aldicarb food poisoning from contaminated melons California. A muscarinic receptor antagonist (MRA) is a type of anticholinergic agent that blocks the … What are some applications for Anticholinergics? Since ciguatoxin is very soluble in fats, its absorption from the intestine is rapid and considerable. Muscarine is the prototypical agonist for all muscarinic receptors (muscarine is an alkaloid derived from mushrooms and is associated with toxicity when poisonous mushrooms are ingested). muscarinic agonistd. Severe muscarinic poisoning can cause _____. Katzung BG: Basic & Clinical Pharmacology, 11e, "Structures of muscarine picrate and muscarine tetraphenylborate", "Pharmacological actions of pure muscarine chloride", Octatropine methylbromide (anisotropine methylbromide), Scopolamine butylbromide (hyoscine butylbromide), Nicotinic acetylcholine receptor modulators, Acetylcholine metabolism/transport modulators, https://en.wikipedia.org/w/index.php?title=Muscarine&oldid=991958895, Pages using collapsible list with both background and text-align in titlestyle, Articles containing unverified chemical infoboxes, Articles needing additional medical references from November 2019, All articles needing additional references, Articles requiring reliable medical sources, Creative Commons Attribution-ShareAlike License, This page was last edited on 2 December 2020, at 18:49. Death after 8 to 9 hours has been reported in about 5% of the cases, but can be avoided completely by prompt diagnosis and treatment with atropine.[21]. Two antidotes are administered to treat organophosphate poisoning. The improper usage of atropine can cause iatrogenic atropine toxicity and in some … The utility of pralidoxime in the treatment of organophosphate poisoning is … Atropine as an anticholinergic act as a competition for acetylcholine at the muscarinic receptors of the body. The structural formula of 2R-muscarine. Atropine is, like muscarine, an alkaloid but unlike muscarine is an antagonist of the muscarinic receptors. Among the thousands of mushroom species identified, few are considered to be edible. Muscarinic agonists activate muscarinic receptors while nicotinic agonists activate nicotine receptors. Used as an antidote to reverse muscle paralysis resulting from OP AChE pesticide poisoning but is not effective once the OP compound has bound AChE irreversibly (aged). Toxicity occurs because of the presence of up to 28 belladonna alkaloids, predominated by … Antimuscarinic drugs are used as antiarrhythmic, antiparkinson, antiasthmatic, and antispasmodic agents, as well as antidote of the natural mushroom alkaloid muscarine (Amanita muscaria) or to prevent parasympathetic stimulation at neuroeffector junctions. Oximes may not reactivate the muscarinic symptoms of organophosphate poisoning [25,26]. Poisoning, overdose, antidotes. Murray DB, Eddleston M, Thomas S, Jefferson RD, Thompson A, Dunn M, et al. Rapid and complete bioavailability of antidotes for organophosphorus nerve agent and cyanide poisoning … Atropine is, like muscarine, an alkaloid but unlike muscarine is an antagonist of the muscarinic receptors. Atropine can cross the blood-brain barrier and can help decrease the activity of centrally acting excess acetylcholine. S-(−)-Ethyl lactate (2)(Figure 4) is converted into the 2,6-dichlorobenzyl ether (3). Chronic atropine poisoning occurs with its long-term use and small overdose. Hence, it inhibits the effects of acetylcholine. Muscarinic antago… MMWR 1986; 35: 254-258. The term antidote is a Greek word meaning “given against”. Physostigmine can be used as an antidote in what type of poisoning? Direct acting muscarinic agonist (binds reversibly to muscarinic cholinergic receptors causing activation) What is the use of bethanechol? [3] 2,5-Anhydro-1,4,6-trideoxy-6-(trimethylammonio)-, InChI=1S/C9H20NO2/c1-7-9(11)5-8(12-7)6-10(2,3)4/h7-9,11H,5-6H2,1-4H3/q+1/t7-,8-,9+/m0/s1, InChI=1/C9H20NO2/c1-7-9(11)5-8(12-7)6-10(2,3)4/h7-9,11H,5-6H2,1-4H3/q+1/t7-,8-,9+/m0/s1, Except where otherwise noted, data are given for materials in their, Please review the contents of the section and. Current recommendation is administration within 48 h of OP poisoning. Picmonic's rapid review multiple-choice quiz allows you to assess your knowledge. Key Points Many medications may have anticholinergic effects and interaction between two or more of these medications can lead to symptoms such as an agitated delirium, mydriasis, dry mouth and tachycardia. Also people with an obstruction in the gastrointestinal or urinary tract are not prescribed muscarine because it will aggravate the obstruction, causing pressure to build up that may lead to perforation. It can be synthesized in various ways from completely different substances,[8][9][10][11][12][13][14][15][16][17] particularly from 2,5-dimethyl-3-carboxymethyl flurane. nicotinic agonistb. Such patients may manifest signs of the antimuscarinic toxidrome resulting from muscarinic receptor blockade. The odd numbered receptors, M1, M3 and M5, interact with Gq proteins to stimulate phosphoinositide hydrolysis and the release of intracellular calcium. Initial gastroenteritis, which may occur 6 to 12 hours after ingestion, can be severe; hypoglycemia can occur. Anon. The antidote for antimuscarinic toxicity is physostigmine salicylate. Atropine acts as a direct antidote physiologically by antagonizing the muscarinic receptor's actions of excessive acetylcholine such as bronchorrhea, bradycardia, salivation, and bronchoconstriction. By inhibiting acetylcholinesterase, there is an increased concentration of acetylcholine which augments stimulation at muscarinic receptors. anticholinergicc. They are also used to treat urinary incontinence and diseases characterized by bowel hypermotility such as irritable bowel syndrome. Explanation for the incorrect answer: Option (a) nicotinic agonist. A few drugs that are derivatives of ACh have proven effective as therapeutic agents, in part because of their resistance to degradation by AChE (see Table 6-5). Mechanism of action in organophosphate poisoning management The exact mechanism by which galantamine protects from organophosphate toxicity is not well established [ 38 ]. Being a quaternary ammonium salt, muscarine is less completely absorbed from the gastrointestinal tract than tertiary amines, and it does not cross the blood-brain barrier. As muscarine works on the muscarinic acetylcholine receptor, the best comparison can be made with acetylcholine, which normally works on this receptor. Of these mushrooms, people with drug dependence are prepared in solutions, causing euphoria and hallucinations. This article have been viewed 722 times. Other muscarinic antagonists are scopolamine and pirenzepine Mild muscarinic toxicities do not require any specific treatment and adequate hydration is good enough in its management. Most agonists for muscarine receptors are not selective for subtypes.[18]. 2. Hence, it inhibits the effects of muscarine. Mechanisms of toxicity. Diisobutylaluminium hydride (DIBAL) reduction of the 2,6-dichlorobenzyl ether gives the aldehyde (4). Filed under Basic Science. Muscarinic antagonist poisoning is characterized by (7) dry mouth; blurred vision; photophobia; hyperthermia; hallucinations and delirium; and skin that is hot, dry, and flushed. Nevertheless, early occurrence of vomiting and diarrhea may facilitate the removal of some amount of the toxin before its absorption (Lehane and Lewis 2000). The most toxic Amanita mushroom is Amanita phalloides, which causes 95% of mushroom poisoning deaths. A poison is any substance that, when ingested, inhaled, absorbed, applied to skin, or produced within the body in relatively small amounts, injures the body by its chemical action. Pilocarpine is an example of a muscarinic agonist. Synopsis. There is no antidote in the case of ciguatoxin poisoning, only adjunct therapy is undertaken. The best antidote for Muscarinic antagonist poisoning is. Muscarinic antagonists (antimuscarinic agents) are a group of anticholinergic drugs that competitively inhibit postganglionic muscarinic receptors.As such, they have a variety of applications that involve the parasympathetic nervous system.Which organ systems are most affected by an antimuscarinic agent depends on the specific characteristics of the agent, particularly its lipophilicity. Signs of mushroom poisoning usually appear within 15-30 minutes of their consumption; Atropine is the standard antidote Remember more in less time and boost your test scores with Picmonic, the world’s best visual mnemonic learning resource and study aid for medical school, nursing school, and more! physostigmine, a cholinesterase inhibitor. [20], Muscarine poisoning is characterized by miosis, blurred vision, increased salivation, excessive sweating, lacrimation, bronchial secretions, bronchoconstriction, bradycardia, abdominal cramping, increased gastric acid secretion, diarrhea and polyuria. … Poisoning with carbamates produces overstimulation of muscarinic and nicotinic receptors, resulting in specific clinical presentations. Since ciguatoxin is very soluble in fats, its absorption from the intestine is rapid and considerable. Administration of the muscarinic antagonist atropine is fundamental to the management of OP poisoning.39 Its action at the synaptic cleft counters the effect of the increased level of acetylcholine in the parasympathetic nervous system, increasing the heart rate and blood pressure and reducing excess fluid and bronchospasm in the lungs. In addition, the specific antidotes atropine and pralidoxime (2-PAM) are employed. The best antidote for Muscarinic antagonist poisoning is. Unlock all 1 facts & definitions with Picmonic Free! Pilocarpine refers to a drug, which is an antidote for atropine poisoning. Antidote for anticholinesterase insecticidal poisoning: (IM or IV): Initial dose: 1 - 2mg is given and dose can be increased up to 6 mg in severe cases and repeat the dose every 5 - 60 minutes until muscarinic symptoms disappears. Antimuscarinic agents block muscarinic receptors (type of ACh receptor) reversing muscarinic effects such as diarrhea, urination, miosis, bronchospasm, bradycardia, skeletal muscle excitation, lacrimation, sweating and salivation. A. muscaria fruitbodies contain a variable dose of muscarine, usually around 0.0003% fresh weight. Muscarinic antagonists are often called parasympatholytics because they have the same effect as agents that block postganglionic parasympatic nerves. Anticholinesterase drugs and blockers of muscarinic cholinergic receptors produce the opposite actions - they excite or inhibit parasympathetic innervation, therefore … Similarly atropine does not have any effects on nicotinic receptors. See also: muscarine , nicotinic . Because it does not significantly relieve depression of respiratory center or decrease muscarinic effects of AChE poisoning, administer atropine concomitantly to block these effects of OP poisoning. See also. The name muscarine derives from that of Amanita muscaria, from which it was first isolated, by German chemists Oswald Schmiedeberg and Richard Koppe at the University of Dorpat, who reported their findings in 1869. Conversely, the even numbered receptors, M2 and M4, interact with Gi proteins to inhibit adenylyl cyclase, which results in a decrease of intracellular concentration of cyclic adenosine monophosphate (cAMP). Mushroom implicated in a fatal ingestion. Atropine is a competitive antagonist of acetylcholine at muscarinic receptors and is used to control the excessive bronchial secretions which are often responsible for death. Atropine refers to a muscarinic receptor, which is obtained from Atropa plant. Therefore, signs and symptoms of antimuscarinic toxicity include flushing, dry skin and mucous membranes, mydriasis, altered mental status and fever. Oral pilocarpine tablets, as well as another muscarinic agent (cevimeline), have recently been approved for the treatment of dry mouth (xerostomia). The antidote for antimuscarinic toxicity is physostigmine salicylate. Thus, the antidote for atropine poisoning cannot be a nicotinic agonist, anticholinergic or α-blocker. Prepared By- Ms. Anshu M.Sc Nursing KGMU Institute of Nursing 2. Gastric and small bowel colic leads to diarrhea, and there is a painful urge for urination. Cardiac ventricles contain muscarinic receptors that mediate a decrease in the force of contractions leading to a lower blood pressure. This is very low and toxicity symptoms occur very rarely. With the exception of the double bonded oxygen, all of the acetylcholine structure is present in the right bottom side of muscarine (see Figure 3 below for comparison of both strtuctures).[6]. 2014 Sep 6. The effective management of poisoning is based upon the use of general supportive measures, reduction of drug absorption or increase in elimination and the use of specific pharmacological agents (‘antidotes’). Severe poisoning leads to seizures, hypotension and collapse. Trace concentrations of muscarine are also found in Amanita muscaria, though the pharmacologically more relevant compound from this mushroom is the Z-drug-like alkaloid muscimol. The best antidote for muscarinic antagonist poisoning is _____, an inhibitor of acetylcholinesterase. There are two mirror forms of muscarine, named: 2S-muscarine and 2R-muscarine. Published on 02/03/2015 by admin. Treatment of the crude aldehyde with allyl bromide and zinc powder in water with NH4Cl as catalyst resulted in an anti:syn mixture of 5a and 5b. A few drugs that are derivatives of ACh have proven effective as therapeutic agents, in part because of their resistance to degradation by AChE (see Table 6-5). The branch of medicine that deals with the detection and treatment of poisons is known as toxicology. [5] These new findings set into motion research on the pharmacology of muscarine and muscarine-like substances that are structurally related to acetylcholine. M1 and M4 subtypes are more abundant in brain and autonomic ganglia. Muscarine is a nonselective agonist of the muscarinic acetylcholine receptors. The medical management of carbamate poisoning consists of supportive measures and specific antidotal treatment, that is, the anticholinergic compound atropine. Finally, it’s an antidote for poisoning by anticholinesterases like organophosphates found in pesticides. Muscarine mimics the function of the natural neurotransmitter acetylcholine in the muscarinic part of the cholinergic nervous system, despite the less flexible structure due to the five-membered ring in the molecular skeleton. They are also used to treat urinary incontinence and diseases characterized by bowel hypermotility such as irritable bowel syndrome. Atropine is a muscarinic receptor blocker, which acts to block the organophosphate-induced over stimulation of central and muscarinic cholinergic nerve terminals. Mushrooms are commercially cultivated over the world and safe for human consumption, except in those with known allergies. Finally, it’s an antidote for poisoning by anticholinesterases like organophosphates found in pesticides. Poisoning may also occur as a result of accidental ingestion, occupational exposure and in the context of recreational substance use. The most likely way for muscarine to leave the blood is via renal clearance; it will eventually leave the body in urine.[19]. [2] The mushroom’s specific name in turn comes from the Latin musca for fly because the mushroom was often used to attract and catch flies, whence also its common name, “fly agaric.”. Current recommendation is administration within 48 h of OP poisoning. This antidote is only available through the Special Access Program. So, the correct answer is option (c). So, the correct answer is option (c). Muscarine was the first parasympathomimetic substance ever studied and causes profound activation of the peripheral parasympathetic nervous system that may end in circulatory collapse and death. [1] Muscarinic receptors also signal via other pathways, for instance via G beta-gamma complex modulation of potassium channels. Search for a specific Video or category now. These agents prolong the effect of acetylcholine by inhibiting their break down, so atropine can help by simply blocking the muscarinic receptors. Other muscarinic antagonists are scopolamine and pirenzepine Mild muscarinic toxicities do not require any specific treatment and adequate hydration is good enough in its management. Pralidoxime does not replace the use of atropine in treating muscarinic signs (e.g. physostigmine; can cross membranes easier . Your rating: none, Average: 0 (0 votes) Rate it. Anticholinesterase drugs and blockers of muscarinic cholinergic receptors produce the opposite actions - they excite or inhibit parasympathetic innervation, therefore they are antidotes for corresponding acute poisonings. An antidote is a substance that can counteract a form of poisoning. Benson B, Tolo D & McIntire M. Is the intermediate syndrome in organophosphate poisoning the result of insufficient oxime therapy? Atropine is a muscarinic antagonist which is derived from Atropa plant. How It Works: Atropine, the Nerve Gas Antidote This ordinary, generic drug has some extraordinary uses, especially when it comes to treating exposure to nerve gases. Atropine is also an alkaloid and inhibits acetylcholine and thus muscarine by binding to muscarinic receptors. Preanesthetic medication, ophthalmic examinations, and reversal of bradycardia. Inocybe and Clitocybe contain muscarine concentrations up to 1.6%.[1]. So, the mode of action as an antidote is to prevent muscarine from binding to the receptor, thus inhibiting its effects on the body. Adverse effects of atropine are... dry mouth, blurred vision, photophobia, tachycardia, urinary retention, constipation, and anhidrosis. The M2 and M3 subtypes mediate muscarinic responses at peripheral autonomic tissues. Muscarinic antagonists (antimuscarinic agents) are a group of anticholinergic drugs that competitively inhibit postganglionic muscarinic receptors.As such, they have a variety of applications that involve the parasympathetic nervous system.Which organ systems are most affected by an antimuscarinic agent depends on the specific characteristics of the agent, particularly its lipophilicity. Copyright © 2020 Picmonic - All Rights Reserved |, We use cookies to offer you a better experience and to analyze site traffic. Discussion: Severe organophosphate poisoning with nicotinic and/or central manifestations should be treated with pralidoxime in addition to atropine. Antimuscarinics such as atropine can be used as an antidote to muscarine. Option (c) muscarinic receptor. Organophosphate toxicity presents as outcomes of muscarinic receptor hyperstimulation: diarrhea, diaphoresis, increased urination, miosis, bronchospasm, bradycardia, emesis, lacrimation, and salivation. These agents prolong the effect of acetylcholine by inhibiting their break down, so atropine can help by simply blocking the muscarinic receptors. Atropine is a specific antidote for the treatment of poisoning with OP and carbamate insecticides and OP nerve agents, acting by competitively blocking the action of excess ACh at muscarinic receptors, and is also used in resuscitation, anaesthesia and ophthalmology. Atropine is also an alkaloid and inhibits acetylcholine and thus muscarine by binding to muscarinic receptors. Muscarine is contraindicated in people with diseases that make them susceptible to parasympathetic stimulation, people who have asthma or COPD, or people who have peptic ulcer disease. A similar reaction sequence with 5b gave (+)-epimuscarine (7).[7]. Muscarinic antagonists dilate the pupil and relax the ciliary muscle, are used in treatment of inflammatory uveitis and is associated with glaucoma. Muscarinic poisoning from medications and mushrooms. 3. Initial symptoms abate for a few days; then liver failure and sometimes renal failure develop. Atropine can also be used for rapid onset mushroom poisoning especially when there is a predominance of muscarinic excess symptoms such as bradycardia, hypotension, rhinorrhea, bronchospasm, respiratory distress, hypersalivation, abdominal cramping, and diarrhea. Figure 2. Poisoning m-holinomimetikami and muscarine Muscarine is an alkaloid of natural origin, which is found in some poisonous mushrooms. Unforgettable characters with concise but impactful videos (2-4 min each). Poisonings - Acute Guidelines for Initial Management Poisonings - Antihistamines / antihistamine-decongestant poisoning Poisonings - Tricyclic antidepressant poisoning. Roberts Bartholow, “A practical treatise on materia medica and therapeutics”, 1908, Peter G. Waser; Chemistry and pharmacology of muscarine, muscarone and some related compounds; Pharmacology Department, University of Zurich, Switzerland 1961, Pappano Achilles J, "Chapter 7. Muscarinic effects by organ system include the following: ... An optimal antidote against organophosphate poisoning. Having a muscarinelike action, that is, producing effects that resemble postganglionic parasympathetic stimulation. We report a 53-year-old woman in Queensland who died from an acute muscarinic syndrome 10 hours after eating mushrooms belonging to the genus Rubinoboletus.To our knowledge, this is the first death in Australia caused by non-amatoxin-producing mushrooms. Both are direct-acting cholinomimetics; they produce their effects by binding to and activating cholinergic receptors. The specific antidote is atropine. The antidote for the muscarinic effects of nerve agents is atropine, which should be given in a dose sufficient to dry respiratory secretions and relax bronchospasm, allowing the victim to be ventilated and oxygenated. These receptors were named after muscarine, to differentiate them from the other acetylcholine receptors (nicotinic receptors), which are comparatively unresponsive to muscarine. Authors Robert G Hendrickson 1 , Anthony P Morocco, Michael I Greenberg. The specific antidote is atropine. This post will help you familiarize yourself with the common antidotes that are used in the hospital setting. Carbamates are acetylcholinesterase inhibitors abundant in various pesticides and they are also used in medicine. 90 Muscarinic Antagonists Uses Antidote for muscarinic agonist poisoning= ATROPINE Parkinson’s Disease (or Pseudo-Parkinsonism) Central acting anticholinergics Hypertensive crises/hypertension Gangionic blockers Neurogenic bladder To decrease spasms. Physostigmine is the only reversible acetylcholinesterase inhibitor capable of directly antagonizing the CNS manifestations of anticholinergic toxicity because it is an uncharged tertiary amine that can efficiently cross the blood brain barrier. Therapeutic Actions for Muscarinic Antagonists: Drug: Organ System. If muscarine reaches the brain it can cause tremor, convulsions and hypothermia. Indicated for urinary retention, GERD, GI paralysis, post-op distention, NOT for use with a physical UT obstruction Muscarine, L-(+)-muscarine, or muscarin is a natural product found in certain mushrooms, particularly in Inocybe and Clitocybe species, such as the deadly C. dealbata. Author information: (1)Department of Medicine, University of Missouri Hospital and Clinics, Columbia 65212. Datura species, especially Datura stramonium (e.g., jimsonweed), are the focus of scores of case reports that chronicle the toxidrome of anticholinergic toxicity. Toxicology. Average : rate 1 star rate 2 star rate 3 star rate 4 star rate 5 star. Patients suspected of, or known to be poisoned by various drugs or plants with antimuscarinic properties may be considered for physostigmine administration. (NCI04) This allows muscarine to modulate cellular excitability via the membrane potential. The antidote for antimuscarinic toxicity is physostigmine salicylate. A paucity of research exists on the metabolism of muscarine in the human body, suggesting this compound is not metabolized by humans. Support for an anticonvulsant action of atropine has been presented by McDonough et al. This antagonist results in the dilation of pupil and blockage of muscarinic receptors in eye. Final proof of the structure was given by Franz Jellinek and colleagues in 1957 with the help of X-ray diffraction analysis;[4] Jellinek further described the three-dimensional structure of the molecule using muscarine chloride. There is no antidote in the case of ciguatoxin poisoning, only adjunct therapy is undertaken. Muscarinic agonists are used as drugs in treating glaucoma, postoperative ileus, congenital megacolon, urinary retention and xerostomia. 2. This can be remembered with the mnemonic "red as a beet, dry as a bone, blind as a bat, mad as a hatter, and hot as a hare." Solution for Which type of drug would be an antidote to atropinepoisoning?a. The antidote for antimuscarinic toxicity is physostigmine salicylate. Treatment of 5a with iodine in CH3CN at 0 °C gives the cyclized product 6a. Muscarinic antagonist: Natural or synthetic Antimuscarinic Agents inhibit acetylcholine neurotransmitter action at muscarinic receptors. Physostigmine is the only reversible acetylcholinesterase inhibitor capable of directly antagonizing the CNS manifestations of anticholinergic toxicity because it is an uncharged tertiary amine that can efficiently cross the blood brain barrier. A puzzling symptom complex. Oral pilocarpine tablets, as well as another muscarinic agent (cevimeline), have recently been approved for the treatment of dry mouth (xerostomia). Pilocarpine is an example of a muscarinic agonist. Option (c) muscarinic receptor. Paediatric dose = 50 micrograms/kg. Pilocarpine refers to a drug, which is an antidote for atropine poisoning. Organophosphate toxicity also causes increased nicotinic receptor hyperstimulation resulting in muscle paralysis. The protective effect of atropine in organophosphate poisoning may therefore be far more than simple muscarinic blockade. Then salivation, lacrimation, and diffuse perspiration set in, combined with miosis, disturbed accommodation, and reduced vision. Prevention of Bronchospasm: 0.025 mg / kg is administered with the help of a nebulisers 3 - 4 times daily up to 2.5 mg Physostigmine is the only reversible acetylcholinesterase inhibitor capable of directly antagonizing the CNS manifestations of anticholinergic toxicity because it is an uncharged tertiary amine that can efficiently cross the blood brain barrier.

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